bluuebunny/crossref_metadata_2025_split huggingface dataset:
Reaction of oligomethylene di(3‐oxobutanoate) with 1,1‐disubstituted alkenes and molecular oxygen in the presence of manganese(II and/or IE) acetate
Authors: Ouyang Jie , Nishino Hiroshi , Kurosawa Kazu 
Published: March 2009

AbstractThe reactions of 1,1‐disubstituted ethenes with oligomethylene di(3‐oxobutanoate) in the presence of manganese(II and/or III) acetate and atmospheric oxygen yielded an ω‐(3‐oxobutanoyloxy)alkyl 6,6‐diaryl‐3‐hydroxy‐3‐methyl‐1,2‐dioxane‐4‐carboxylate, oligomethylene di(6,6‐diaryl‐3‐hydroxy‐3‐methyl‐1,2‐dioxane‐4‐carboxylate)s, ω‐hydroxyalkyl 6,6‐diaryl‐3‐hydroxy‐3‐methyl‐1,2‐dioxane‐4‐carboxylates, an ω‐(3‐oxobutanoyloxy)alkyl 5,5‐diaryl‐2‐methyl‐4,5‐dihydrofuran‐3‐carboxylate, oligomethylene di(5,5‐diaryl‐2‐methyl‐4,5‐dihydrofuran‐3‐carboxylate)s, ω‐hydroxyalkyl 5,5‐diaryl‐2‐methyl‐4,5‐dihydrofuran‐3‐carboxylates, and an ohgomethylene diester bearing a substituted 1,2‐dioxane ring and a substituted 4,5‐dihydrofuran ring. The reaction of the 1,2‐dioxan‐3‐ols with acid gave the corresponding compounds bearing furan rings. The reaction of 1,1,6,6‐tetraaryl‐1,5‐hexadienes with oligomethylene di(3‐oxobutanoate) in the presence of manganese(III) acetate yielded macrocyclic diesters bearing two 4,5‐dihydrofuran rings.
New access to 4‐phenyl‐6H‐pyrrolo[1,2‐a]thieno[3,2‐f]‐[1,4]diazepines
Authors: Foloppe Marie‐Paule , Sonnet Pascal , Bureau Isabelle , Rault Sylvain , Robba Max 
Published: March 2009

AbstractPyrrolo[1,2‐a]thieno[3,2‐f][1,4]diazepines were obtained in an original one step synthesis by treatment of imines 1 with paraformaldehyde in refluxing ethanol. The intermediate Mannich bases were also converted into the thienooxadiazocines 12 and the diazepine N‐oxide 13.
5‐(α‐Fluorovinyl)tryptamines and 5‐(α‐Fluorovinyl)‐3‐(N‐methyl‐1′,2′,5′,6′,‐tetrahydropyridin‐3′‐ and ‐4′‐yl)indoles—5‐(α‐Fluorovinyl)tryptamines
Authors: Gharat Laxmikant A. , Martin Arnold R. 
Published: March 2009

Abstract5‐(α‐Fluorovinyl)tryptamines 4a, 4b and 5‐(α‐fluorovinyl)‐3‐(N‐methyl‐1′,2′,5′,6′‐tetrahydropyridin‐3′‐ and ‐4′‐yl) indoles 5a, 5b were synthesized using 5‐(α‐fluorovinyl)indole (7). The target compounds are bioisosteres of 5‐carboxyamido substituted tryptamines and their tetrahydropyridyl analogs.
Synthesis of new azepino[3,4,5‐cd]indole derivatives
Authors: Hayes J. F. , Hayler J. D. , Walsgrove T. C. , Wicks C. 
Published: March 2009

AbstractNew 2‐oxoazepino[3,4,5‐cd]indole derivatives were formed by the reaction of the tosylate SK&F 98339 with N‐alkyl and N‐arylidenepropylamines in moderate yield.
An unusual formation of 1H‐s‐triazole N‐imines from reactions of 1,3,4‐oxadiazin‐6‐ones and nitrilimines
Authors: Argyropoulos Nikolaos G. , Corobili Ecaterini , Raptopoulou Ecaterini P. 
Published: March 2009

AbstractA new, unusual way to obtain polysubstituted 1H‐S‐triazole N‐imine derivatives is described from reactions of the readily available 1,3,4‐oxadiadin‐6‐one derivatives and nitrilimines. Besides an hydrazide derivative of phenylglyoxylic acid is also formed. Both adducts were characterised by X‐ray crystal structure analysis.
1,4‐Benzoxazin‐2‐ones, benzo[d]oxazoles and 2H‐1,4‐benzoxazines from the reaction of 2‐(methoxyimino)benzen‐1‐ones with arylacetates, arylacetic acids and trans‐ stilbene
Authors: Nicolaides Demetrios N. , Awad R. Wajih , Varella Evangelia A. 
Published: March 2009

Abstract10‐(Methoxyimino)phenanthrene‐9‐one 1 reacts thermally with the arylacetic derivatives 2(a‐j) to yield the corresponding 1,4‐benzoxazin‐2‐ones 4(a‐d,f) and benzo[d]oxazoles 5(a‐e,g). Similarly, reaction of the monoximes 7a, 7b with compounds 2a, 2d respectively affords 8a, 8b, while action of trans‐stilbene on the monoximes 1, 7a, 7b leads to the 1,4‐benzoxazines 10, 11, 13, obtained along with the corresponding 2‐phenyloxazoles 5a, 8a, 8c and compound 12.
Transformations of the pyrido[1,2‐a]pyrazine ring system into imidazo[1,2‐a]pyridines, imidazo[1,2‐a]pyrimidines and 2‐oxa‐6a, 10c‐diazaaceanthrylenes
Authors: Kolar Patrik , Tišler Miha , Pizzioli Alessandro 
Published: March 2009

AbstractTransformations of methyl 3‐dimethylamino‐2‐(1‐methoxycarbonyl‐4‐oxo‐4H‐pyrido[1,2‐a]pyrazin‐3‐yl)acrylate with some cyanomethylenecarbonyl group containing compounds or cyanamide into imidazo‐[1,2‐a]pyridines, irmdazo[1,2‐a]pyrimidines and 2‐oxa‐6a, 10c‐diazaaceanthrylenes are described.
17O NMR studies of electronic and steric interactions of substituted quinoxaline‐2(1H),3(4H)‐diones
Authors: Gerothanassis Ioannis P. , Varvounis George 
Published: March 2009

Abstract17O nmr studies, at natural abundance, of substituted quinoxaline‐2(1H),3(4H)‐diones demonstrate that the 17O chemical shift data can provide new insights into steric and electronic interactions due to long range substituent effects on the aromatic ring. The role of considerable “keto” character and torsion angle deformation of the diamide group in solution is emphasized.
Adducts of phenanthrene 9,10‐imine and of benz[a]anthracene 5,6‐imine to some nitrogen heterocycles
Authors: Shalom Yosef , Blum Jochanan , Harvey Ronald G. 
Published: March 2009

AbstractN‐4‐Pyridinyl‐, N‐2‐quinolinyl‐, and 2‐pyrazinylphenanthrene 9,10‐imines 4–6, as well as N‐4‐pyridinyl‐ and N‐2‐pyrazinylbenz[a]anthracene 5,6‐imines 12 and 13 were prepared by sodium hydride‐mediated interaction of the parent arene imines, 1 and 10, and the respective chloropyridine, chloroquinoline or chloropyrazine. N‐Nicotynoyl‐, N‐2‐pyridinoyl‐ and N‐6‐quinolinoylphenanthrene 9,10‐imines 7–9 were obtained by interaction of N‐trimethylsilylphenanthrene 9,10‐imine (2) and the appropriate pyridine‐ or quinolinecarbonyl chlorides. Reaction of N‐methylsulfonylphenanthrene 9,10‐imine with thymine, cytosine, 5‐fluorocytosine, purine, 6‐chloropurine and adenine afforded, in the presence of either potassium carbonate or 1,5‐diazabicyclo[3.4.0]non‐5‐ene, adducts 16–22, respectively. The structures of the adducts were conformed by multinuclear nmr and by NOESY and C‐H correlation 2D nmr spectrometry.
Aminonitropyridines and their N‐oxides
Authors: Hollins Richard A. , Merwin Lawrence H. , Nissan Robin A. , Wilson William S. , Gilardi Richard 
Published: March 2009

Abstract2,6‐Diamino‐3,5‐dinitropyridine 1‐oxide has been prepared by mixed acid nitration of 2,6‐diaminopyridine, followed by oxidation using hydrogen peroxide in acetic acid. 3,5‐Dinitro‐2,4,6‐triaminopyridine has been prepared by oxidative amination of 2‐chloro‐3,5‐dinitropyridine or 2,6‐diamino‐3,5‐dinitropyridine using potassium permanganate in liquid ammonia, or by “vicarious nucleophilic amination” of 2,6‐diarnino‐3,5‐dinitropyridine using hydroxylamine in aqueous potassium hydroxide. 3,5‐Dinitro‐2,4,6‐triaminopyridine 1‐oxide has been prepared by oxidation of 3,5‐dinitro‐2,4,6‐triaminopyridine using hydrogen peroxide in acetic acid, and by “vicarious nucleophilic amination” of 2,6‐diamino‐3,5‐dinitropyridine 1‐oxide. Nmr spectroscopy and single crystal X‐ray diffraction studies have shown that these compounds have the planar structures and intra‐ and inter‐molecular hydrogen bonding necessary to confer on the materials the high density, the thermal and chemical stability, and the explosive insensitivity required for new insensitive energetic materials.
Synthesis and structure elucidation of new cytotoxic azathioxanthones
Authors: Varvaresou A. , Tsotinis A. , Papadaki‐Valiraki A. , Siatra‐Papastaikoudi Th. 
Published: March 2009

AbstractA series of new cytotoxic azathioxanthones 7a‐h was synthesized and characterized by their spectral data.
Efficient syntheses and crystal structures of new benzene‐containing cryptands
Authors: Bordunov Andrei V. , Dalley N. Kent , Kou X. , Bradshaw Jerald S. , Pastushok Victor N. 
Published: March 2009

AbstractSeven new cryptands 3–9 containing two or three aromatic rings in one bridge were prepared in good yields by treating N,N'‐bis(p‐chlorophenol)‐substituted diaza‐18‐crown‐6 (2) with three oligoethylene glycol ditosylates, 1,3‐propanediol ditosylate, 2,6‐pyridinedimethanol ditosylate, α,α'‐dibromo‐o‐xylene and α,α'‐dibromo‐p‐xylene. Because of the convenient synthesis of 2 from N,N'‐bis(methoxymethyl)diaza‐18‐crown‐6 (1) and the relative ease of isolation of the cryptand products, this is an excellent method for the design of three‐dimensional cavities containing aromatic fragments. In an attempt to better understand the synthetic route to the cryptands, the crystal structures of KI·2 and Na Picrate·2 were determined using X‐ray analysis. In addition, crystal structure analyses of cryptands 3, 6 and 8 were used to establish their structures.
Pyrimidines. XXXIII. Synthesis and properties of new fervenulin derivatives
Authors: Werner‐Simon Susanne , Pfleiderer Wolfgang 
Published: March 2009

AbstractA series of new 3‐substituted fervenulin (6,8‐dimethylpyrimido[5,4‐c]‐1,2,4‐triazine‐5,7‐dione) (1) derivatives have been synthesized by modifying the 3‐alkyl‐ and aralkyl side‐chains. Brominations of 3‐methyl‐15, 3‐ethyl‐16‐ and 3‐benzylfervenulin (17) led to mono‐ and dibromo derivatives 22, 23, 25–27, which are prone to various nucleophilic displacement reactions 24, 28–35. Periodate oxidation and ozonolysis, respectively, of 3‐styrylfervenulin (20) afforded fervenulin‐3‐carboxaldehyde (36) which was transformed to a folic acid analog (39). Potassium permanganate oxidation of 3‐alkylfervenulins 15–19 afforded only ring‐contraction to 3‐alkyl‐5,7‐dimethylimidazo[4,5‐e]‐1,2,4‐triazin‐6‐ones 42–46 which are also formed as mixtures with its 2,4a‐dihydro derivatives 47–50 on treatment with ethanolic sodium hydroxide. Fervenulin‐3‐carboxylic acid (55) can be converted to the corresponding acid chloride 58 which reacts with amines to fervenulin‐3‐carboxamides 59, 64–67 and/or 2,4a‐dihydro‐5,7‐dimethylimidazo[4,5‐e]‐1,2,4‐triazin‐6‐one‐biscarboxamides 60–64.
9‐Substituted acridines. Demethoxylation of 9‐methoxyacridine and dechlorination of 9‐chloroacridine in hydroxylic solvents
Authors: Kalatzis Evangelos , Konga Zoi , Geronikolou Konstantina 
Published: March 2009

AbstractIn methanol‐water mixtures containing sodium or potassium hydroxide (up to 2.00M) the demethoxylation of 9‐methoxyacridine to 9‐acridone is of first order in both the free form of 9‐methoxyacridine and the hydroxyl ion. The rate of the reaction is increased with an increase in the concentration of water. Sodium perchlorate has a small retarding effect on the reaction. In methanol‐water mixtures containing perchloric or hydrochloric acid (up to 3.45M) the demethoxylation is of first order with respect to the protonated form of 9‐methoxyacridine. The rate of the reaction decreases with an increase in the concentration of the acid or of sodium perchlorate, but when the concentration of water is increased (≈︁1.7 to 50M) and that of the acid is not changed, it reaches a maximum value in mixtures containing 8 to 10M‐water. The dechlorination of 9‐chloroacridine to 9‐methoxyacridine in methanol containing sodium hydroxide or methoxide (up to 0.31 M) is of first order in both the 9‐chloroacridine and the hydroxyl or methoxyl ions.
Synthesis and biological evaluation of some 4‐(isoxazolinyl or 1,2,4‐oxadiazolyl) coumarins
Authors: Nicolaides Demetrios N. , Fylaktakidou Konstantina C. , Litinas Konstantinos E. , Hadjipavlou‐Litina Dimitra 
Published: March 2009

AbstractReaction of compound 3 with nitrile oxide 4a affords compounds 5a and 6 in 73% and 3% yield respectively, while reaction of 3 with 4b affords only compound 5b (85%). Reactions of compound 8 with the nitrile oxides 4a,b result in compounds 9a,b. The compound 10, prepared from 1 and O‐methylhydroxylamine, reacts with nitrile oxide 4b to give the oxadiazole derivative 12. The above referred coumarins are screened for antiinflammatory activity in vivo using the carrageenin rat paw edema and in vitro through their antiproteolytic activity and their ability to inhibit β‐glucuronidase and 12‐Lipoxygenase.
A novel photoaddition of 2‐phenylbenzimidazole
Authors: Jones Richard H. , Ramsden Christopher A. , Rose Helen L. 
Published: March 2009

AbstractIrradiation of 2‐phenylbenzimidazole (3) in the presence of methyl acrylate (20 equivalents) using a medium pressure mercury lamp gives methyl 2‐(2‐phenylbenzimidazol‐1‐yl)propionate (4) (75%) whose structure has been confirmed by an X‐ray analysis. A similar reaction using acrylonitrile gave only a low yield (1%) of the corresponding propionitrile derivative 5. A mechanism involving photoexcitation of 2‐phenylbenzimidazole (3) followed by sequential single electron transfer, proton transfer and radical coupling is proposed to account for the formation of the novel photoadducts 4 and 5.
Furopyridines. XVII. Cyanation, chlorination and nitration of furo[3,2‐b]pyridine N‐oxide
Authors: Shiotani Shunsaku , Taniguchi Katsunori 
Published: March 2009

AbstractThe N‐oxide 2 of furo[3,2‐b]pyridine (1) was cyanated by the Reissert‐Henze reaction with potassium cyanide and benzoyl chloride to give 5‐cyano derivative 3, which was converted to the carboxamide 4, carboxylic acid 5, ethyl ester 6 and ethyl imidate 8. Chlorination of 2 with phosphorus oxychloride yielded 2‐9a, 3‐ 9b, 5‐ 9c and 7‐chloro derivative 9d. Reaction of 9d with sodium methoxide, pyrrolidine, N,N‐dimethylformamide and ethyl cyanoacetate afforded 7‐methoxy‐ 10, 7‐(1‐pyrrolidyl)‐ 11 and 7‐dimethylaminofuro[3,2‐b]pyridine (14) and 7‐(1‐cyano‐1‐ethoxy‐carbonyl)methylene‐4,7‐dihydrofuro[3,2‐b]pyridine (12). Nitration of 2 with a mixture of fuming nitric acid and sulfuric acid gave 2‐nitrofuro[3,2‐b]pyridine N‐oxide (15).
Studies on pyrrolidinones. synthesis of N‐(2‐nitrobenzyl)pyroglutamic acid
Authors: Rigo BenoǏT , Dolaine RÉGis , Ghammarti Samira El , Couturier Daniel 
Published: March 2009

AbstractWhile methyl N‐(4‐nitrobenzyl)pyroglutamate can be obtained from methyl N‐trimethylsilylpyroglutamate, the best way to obtain methyl N‐(2‐nitrobenzyl)pyroglutamate is to react 4‐nitro benzyl bromide with the iminoether derived from methyl pyroglutamate.
Haloacetylated enol ethers. 6 [5]. Synthesis of 4,5‐trimethylene‐4,5‐dihydroisoxazoles
Authors: Martins Marcos A. P. , Flores Alex F. C. , Freitag Rogério A. , Zanatta Nilo 
Published: March 2009

AbstractThe investigation of the effect of the cyclopentane ring on the regiochemistry of the reactions of 2‐acetylcyclopentanones 1a‐d and β‐methoxyvinyl trifluoromethyl ketone derivative 2a with hydroxylamine hydrochloride is reported. The reactions give regiospecifically the 4,5‐trimethylene‐4,5‐dihydroisoxazoles 3a‐d in good yields.
Synthesis of some 6‐S‐heterocyclic derivatives of 1,2:3,4‐di‐O‐isopropylidene‐α‐D‐galactopyranose
Authors: Alho M. A. Martins , D'Accorso N. B. , Thiel I. M. E. 
Published: March 2009

AbstractWe applied nucleophilic substitution to 6‐O‐tosyl‐1,2:3,4‐di‐O‐isopropylidene‐α‐D‐galactopyranose using sulphur nucleophiles and obtained 6‐S‐derivatives of 1,2:3,4‐di‐O‐isopropylidene‐α‐D‐galactopyranose. We present the physical and spectroscopic characterization of these heterocyclic compounds as well as other related compounds obtained by substitution, using other substrates. The conformational studies of all products are presented and discussed.
Synthesis and characterization of new 1,1′‐diester, diketone, and dinitrile derivatives of 2,2′‐biimidazole
Authors: Barnett Mark , Secondo Paula , Collier Harvest 
Published: March 2009

AbstractSubstituted 1,1′‐diester, diketone and dinitrile derivatives are prepared from 2,2′‐biimidazole. The reactions involved include: Michael addition with halogenated olefins; nucleophilic substitution with ketones, nitriles, and esters; and condensation with amines.
Synthesis of [1,3,4]thiadiazolo[3,2‐a]pyrimidines in the presence of formic acid
Authors: Takenaka Keiko , Tsuji Tadakazu 
Published: March 2009

AbstractFormic acid‐phosphorus pentoxide was effective for the preparation of 5,7‐dimethyl[1,3,4]thiadiazolo‐ and ‐[1,3]thiazolo[3,2‐a]pyrimidin‐4‐ium salts. Further, the pyrimidine ring transformation and the isocyanation of 5imino‐6H‐[1,3,4]thiadiazolo‐ and ‐[1,3]thiazolo[3,2‐a]pyrimidin‐7‐ones were carried out in the presence of formic acid and triethyl orthoformate, respectively.
Alkylation of non‐electron rich nitrogen heterocycles by alkyl orthoformates: Quantum chemistry calculations
Authors: Guccione Salvatore , Russo Filippo , Langer Thierry 
Published: March 2009

AbstractResults of semiempirical MO calculations of N1‐ and N2‐alkyl pyrazolotriazolopyrimidin‐4‐ones originating from alkylation by trimethyl and triethyl orthoformate are presented.
Synthesis of 3‐glycosyl‐5‐substituted‐2‐isoxazolines
Authors: Fascio Mirta L. , D'Accorso Norma B. 
Published: March 2009

AbstractThe synthesis of eight 3‐glycosyl‐5‐substituted‐2‐isoxazolines is described. They are obtained by 1,3‐dipolar cycloaddition from some 2‐deoxy‐sugar oximes. A side product was isolated. The physical and spectroscopycal characterization of all compounds are reported.
Reaction of 4,5‐dichloro‐3‐nitropyridazin‐6‐one with dimethylchloromethyleneammonium chloride
Authors: Kweon Deok‐Heon , Cho Su‐Dong , Kirn Sung‐Kyu , Chung Joo‐Wha , Yoon Yong‐Jin 
Published: March 2009

Abstract3,4,5‐Trichloropyridazin‐6‐one, 3,4,5,6‐tetrachloropyridzine and 4,5‐dichloro‐3‐(N,N‐dimethylamino)‐pyridazin‐6‐one were synthesized from 4,5‐dichloro‐3‐nitropyridazin‐6‐one and dimethylchloromethylene‐ammonium chloride selectively.
Saturated heterocycles. 242. Synthesis of 2‐substituted‐6‐(6′,7′‐dimethoxy‐3′,4′‐dihydro‐1′‐isoquinolyl)‐5,6,7,8‐tetrahydro‐ quinazolin‐4(3H)‐one Derivatives
Authors: Bernáth Gábor , Lázár János , Fülöp Ferenc , Kóbor Jenó 
Published: March 2009

AbstractIn the reactions of the recently synthesized β‐ketoesters 1‐[(3′‐methoxycarbonyl‐ and 1‐[(3′‐ethoxycarbonyl‐4′‐oxo)‐1′‐cyclohexyl]‐3,4‐dihydroisoquinoline 4, 5 with amidines or cyclic guanidines, a number of 2‐substituted‐6‐(6′,7′‐dimethoxy‐3′,4′‐dihydro‐1′‐isoquinolyl)‐5,6,7,8‐tetrahydroquinazolin‐4(3H)‐one derivatives 6–8 were prepared. The new compounds possess various pharmacological actions.
Novel pyrrole‐annulated heterocyclic systems. Synthesis of 10H‐pyrrolo[1,2‐b][1,2,6]benzothiadiazocin‐11(12H)‐one 5,5‐dioxide
Authors: Santo Roberto Di , Costi Roberta , Artico Marino , Massa Silvio 
Published: March 2009

AbstractIntramolecular cyclization of 1‐(2‐aminophenylsulfonyl)‐1H‐pyrrole‐2‐acetic acid 5 gave 10H‐pyirolo[1,2‐b][1,2,6]benzothiadiazocin‐11(12H)‐one 5,5‐dioxide 4, a novel heterocyclic system of pyrrolobenzothiadiazocine family. Compound 5 was obtained starting from 2‐nitrobenzenesulfonyl chloride with ethyl 1H‐pyrrole‐2‐(α‐oxo)acetate, which were condensed to afford 1‐(2‐nitrophenylsulfonyl)‐1H‐pyrrole‐2‐(α‐oxo)acetate 13. Reduction of 13 gave the amino ester 7, which was hydrolyzed to the required aminoacid 5. The synthesis of 7‐chloro‐10H‐pyrrolo[1,2‐b][1,2,6]benzothiadiazocin‐11(12H)‐one 5,5‐dioxide 16 is also described.
Stereoselective synthesis of 2β‐carbomethoxy‐3β‐phenyltropane derivatives. Enhanced stereoselectivity observed for the conjugate addition reaction of phenylmagnesium bromide derivatives with anhydro dichloromethane
Authors: Xu Lifen , Trudell Mark L. 
Published: March 2009

AbstractThe use of dichloromethane as a solvent for the conjugate addition reaction of preformed etheral solutions of phenylmagnesium bromide derivatives with anhydroecgonine methyl ester (2) was found to enhance the stereoselectivity of the reaction and provide the 2β‐carbomethoxy‐3β‐phenyltropane derivatives 3a‐d in high yield.
Synthesis of a 9‐acridinyl nonapeptide containing the DNA recognizing region of 434 phage repressor protein
Authors: Takenaka Shigeori , Iwamasa Kenji , Takagi Makoto , Nishino Norikazu , Mihara Hisakazu , Fujimoto Tutomu 
Published: March 2009

AbstractA peptide‐intercalator conjugate was synthesized by connecting acridine with a Gln‐Gln‐Ser‐Ile‐Glu‐Gln‐Leu‐Glu‐Asn sequence representing the DNA recognizing region of 434 phage repressor protein. This conjugate 7 binds to DNA in spite of its anionic character with the aid of the intercalator.
Synthesis of new dihydrooxathiino[2,3‐b]quinoline
Authors: Hahn Hoh‐Gyu , Chang Kee Hyuk , Lee Wha Suk , Yoo Ji Uk 
Published: March 2009

AbstractA synthesis of new dihydrooxathiinoquinoline 4 is described. The key compound 6 was prepared by known methods from acetoacetanilide 1. A condensation of β‐chlorosulfide 6 in 75% aqueous sulfuric acid gave quinolone 5. Conversion of 5 to 4 was achieved by treatment with potassium hydroxide in ethanol solution.
2,4,6‐trichloropyrimidine. Reaction with 4‐substituted phenolate ions
Authors: Delia Thomas J. , Nagarajan A. 
Published: March 2009

AbstractA systematic investigation of the reactivity of 2,4,6‐trichloropyrimidine with phenoxide nucleophiles has been conducted. Conditions have been described which lead to mono‐, di‐, and trisubstituted‐pyrimidines. Unexpected product distributions for mono‐ and disubstituted products were observed and explanations for these results are offered.
Synthesis and central nervous system stimulant activity of 5,8‐methanoquinazolines fused with 1,2,4‐triazole, tetrazoleand 1,2,4‐triazine
Authors: Nagai Shin‐Icbi , Ueda Taisei , Sugiura Satoe , Nagatsu Akito , Murakami Nobutoshi , Sakakibara Jinsaku , Fujita Michiko , Hotta Yoshiki 
Published: March 2009

Abstract5,8‐Methanoquinazolines fused with 1,2,4‐triazole 4–5, tetrazole 6, and 1,2,4‐triazine 8 were prepared starting from 2‐hydrazino‐5,8‐methanoquinazoline 3. Compound 3 and 6 showed the most potent central nervous system (CNS) stimulant activities.
Reaction of 5‐aminopyrazoles with β‐dimethylaminopropiophenones. Synthesis of new pyrazolo[3,4‐b]pyridines
Authors: Quiroga J. , Insuasty B. , Cruz S. , Hernandez P. , Bolaños A. , Moreno R. , Hormaza Angelina , de Almeida Regina H. S. 
Published: March 2009

AbstractSeveral new pyrazolo[3,4‐b]pyridines were obtained from the reaction of 5‐amino‐1‐aryl‐3‐methylpyrazoles 1 with β‐dimemylaminopropiophenones 2 in pyridine. The structure elucidation of 4,5‐dihydropyrazolo[3,4‐b]pyridines 3 is based on nmr measurements and X‐ray diffraction. The treatment of compounds 3 with N‐bromosuccinimide led to the formation of pyrazolo[3,4‐b]pyridines 4.
Reaction of N1,N2‐diarylacetamidines with (2,4,7‐trinitro‐9H‐fluoren‐9‐ylidene)propanedinitriles
Authors: Gomaa Mohsen Abdel‐Motaal , Döpp Dietrich 
Published: March 2009

AbstractNovel spiro[fluorene‐9,4′‐(1′,2′,3′,4′‐tetrahydropyridine)]‐5′‐carbonitriles 6a‐c have been obtained from the reaction of N1,N2‐diarylacetamidines 1a‐c with (2,4,7‐trinitro‐9H‐fluoren‐9‐ylidene)propanedinitrile (2) in ethyl acetate solutions at ambient temperature for 6a,b or under reflux for 6c, respectively.
Synthesis of 1‐methyl‐7‐(trifluoromethyl)‐1H‐pyrido[2,3‐c][1,2]thiazin‐4(3H)‐one 2,2‐dioxide
Authors: Coppo Frank T. , Fawzi Maged M. 
Published: March 2009

AbstractThe reaction of methyl 2‐bromo‐6‐(trifluoromethyl)‐3‐pyridinecarboxylate (1) with methanesulfonamide gave methyl 2‐[(methylsulfonyl)amino]‐6‐(trifluoromethyl)‐3‐pyridine‐carboxylate (2). Alkylation of compound 2 with methyl iodide followed by cyclization of the resulting methyl 2‐[methyl(methylsulfonyl)amino]‐6‐(trifluoromethyl)‐3‐pyridinecarboxylate (3) yielded 1‐methyl‐7‐(trifluoromethyl)‐1H‐pyrido[2,3‐c][1,2]thiazin‐4(3H)‐one 2,2‐dioxide (4). The reaction of compound 4 with α,2,4‐trichlorotoluene, methyl bromopropionate, methyl iodide, 3‐trifluoromethylphenyl isocyanate, phenyl isocyanate and 2,4‐dichloro‐5‐(2‐propynyloxy)phenyl isothiocyanate gave, respectively, 4‐[(2,4‐dichlorophenyl)methoxy]‐1‐methyl‐7‐(trifluoromethyl)‐1H‐pyrido[2,3‐c][1,2]thiazine 2,2‐dioxide (5), methyl 2‐[[1‐methyl‐2,2‐dioxido‐7‐(trifluoromethyl)‐1H‐pyrido[2,3‐c][1,2]thiazin‐4‐yl]oxy]propanoate (6), 1,3,3‐trimethyl‐7‐(trifluoromethyl)‐1H‐pyrido[2,3‐c][1,2]thiazin‐4(3H)‐one 2,2‐dioxide (7), 4‐hydroxy‐1‐methyl‐7‐(trifluoromethyl)‐N‐[3‐(trifluoromethyl)phenyl]‐1H‐pyrido[2,3‐c][1,2]thiazine‐3‐carboxamide 2,2‐dioxide (8), 4‐hydroxy‐1‐methyl‐7‐(trifluoromethyl)‐N‐phenyl‐1H‐pyrido[2,3‐c][1,2]thiazine‐3‐carboxamide 2,2‐dioxide (9) and N‐[2,4‐dichloro‐5‐(2‐propynyloxy)phenyl]‐4‐hydroxy‐1‐methyl‐7‐(trifluoromethyl)‐1H‐pyrido[2,3‐c][1,2] thiazine‐3‐carboxamide 2,2‐dioxide (10).