bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis of pyridazino[4,5‐b]indole derivatives from 2‐(3‐carboxy‐1‐methylindole)acetic acid anhydride
Authors: Monge A. , Palop J. A. , Goñi T. , Fernández‐Alvarez E. 
Published: March 2009

Abstract2‐(3‐Carboxy‐1‐methylindole)acetic acid anhydride (1) reacts with aryldiazonium salts to give 85–95% of the corresponding α‐hydrazono anhydrides 2. Treating 2 with boiling hydrazine hydrate in xylene, the respective 2‐aryl‐4‐carbohydrazido‐5‐methyl‐1‐oxo‐1,2‐dihydro‐5H/‐pyridazino[4,5‐b]indoles 3 were obtained (47–67%), and these compounds characterized as the respective benzylidene derivatives 4. Compounds 2 react with amines (aniline, morpholine, piperidine) to give the respective 2‐(3‐carboxy‐1‐methylindole)aceta‐mide 5 or the respective 2‐aryl‐4‐carboxamido‐5‐methyl‐5H‐pyridazino[4,5‐b]indole 6, the product obtained depending on the structure of the aryl substituent. Boiling 2b (aryl = 4‐chlorophenyl) with 5% sodium hydroxide gave (80%) 2‐(3‐carboxy‐1‐methylindole)acetic acid (7). Hydrolysis of 2b gave a mixture of 7 and 2‐(3‐carboxy‐1‐methylindolyl)‐2‐(4‐chlorophenylhydrazono)acetic acid (8).
The fragmentation of 7‐(o‐ and p‐R‐benzylidene)‐3‐(o‐ and p‐R‐phenyl)‐2‐methyl‐3,3a,4,5,6,7‐hexahydro‐2H‐indazoles under electron impact. II
Authors: Cortés E. , Martínez R. , Arzacoya E. 
Published: March 2009

AbstractThe electron impact mass spectrometric fragmentation pathways for several 2‐methylindazoles, II, were investigated. Our investigation of the mass spectra of these compounds revealed interesting relationships between the 2‐N‐methyl‐substituent in the framework of II and the fragmentation patterns.
The chemistry of 2H‐3,1‐benzoxazine‐2,4(1H)‐dione (Isatoic Anhydride). 19. Direct formation of 2‐aminobenzyl alcohols from the reduction of N‐substituted isatoic anhydrides
Authors: Coppola Gary M. 
Published: March 2009

AbstractIsatoic anhydrides 1 are easily reduced with sodium borohydride to o‐(substituted‐amino)benzyl alcohols 3 in good yield. Sequential reduction of N‐(2‐nitrobenzyl)isatoic anhydride (5) with sodium borohydride followed by catalytic hydrogenation of the nitro group affords the naturally occurring 2‐(2′‐aminobenzylamino)‐benzyl alcohol (4) in 72% yield.
A conveneint synthesis of 1‐substituted‐2,5(4H)‐piperazinediones
Authors: Lovelette C. A. , Geagan K. 
Published: March 2009

Abstract1‐Substituted‐2,5(4H)‐piperazinediones are prepared by the Michael addition of acrylonitrile and methyl‐acrylate and glycylglycine, DL‐alanyl‐DL‐alanine and DL‐alanyl‐DL‐phenylalanine followed by cyclohydration in refluxing xylenes.
Synthesis of sulfur and nitrogen analogues of monooxo crown ethers
Authors: Matsushima Kenji , Nakatsuji Yohji , Kawamura Norio , Okahara Mitsuo 
Published: March 2009

AbstractSulfur or nitrogen analogues of monooxo crown ethers were prepared via intramolecular cyclization of the corresponding thia or aza oligoethylene glycol carboxylmethyl ethers by using benzenesulfonyl chloride in the presence of alkali metal carbonates.
Synthesis of ribonucleosides of 4(5)‐cyano‐5(4)‐methylimidazole and related 4‐substituted‐5‐methylimidazole ribosides
Authors: Andrés J. Ignacio , García‐Lopez M. Teresa 
Published: March 2009

Abstract4‐Cyano‐1‐(2,3,5‐tri‐O‐acetyl‐β‐D‐ribofuranosyl)‐5‐methylimidazole (4) and its corresponding 5‐cyano‐4‐methyl substituted isomer (5) have been obtained by ribosylation of 4(5)‐cyano‐5(4)‐methylimidazole (3) via the mercuric cyanide method or by ribosylation of the trimethylsilyl derivative of 3. Treatment of 4 with methanolic ammonia, ammonium chloride in liquid ammonia and potassium hydrosulfide provided 4‐cyano‐1‐β‐D‐ribofuranosyl‐5‐methylimidazole (6), 1‐β‐D‐ribofuranosyl‐5‐methylimidazole‐4‐carboxamide (2) and 1‐β‐D‐ribofuranosyl‐5‐methylimidazole‐4‐thiocarboxamide (11) respectively. Reaction of 6 with hydroxylamine afforded the corresponding 4‐carboxamidoxime substituted nucleoside (13) which on catalytic reduction in the presence of ammonium chloride, was transformed into 1‐β‐D‐ribofuranosyl‐5‐methylimidazole‐4‐carboxamidine (14) as hydrochloride salt.
Chemistry of the phenoxathiins and isosterically related heterocycles. XXXII . The synthesis of 2‐azathianthrene and selected analogs
Authors: Lam Wing W. , Martin Gary E. , Lynch Vincent M. , Simonsen Stanley H. , Lindsay Charles M. , Smith Keith 
Published: March 2009

AbstractThe synthesis of 2‐azathianthrene ([1,4]benzodithiino[2,3‐c]pyridine), the only remaining monoazathianthrene yet to be reported, is described. Attempts at the direct condensation of disubstituted pyridines with the dianion of 1,2‐dimercaptobenzene were generally unsuccessful requiring that the alternative condensation of the dianion with disubstituted pyridine 1‐oxides be employed. The title compound was characterized by physical means including 13C‐nmr spectroscopy. One analog, 4‐nitro‐2‐azathianthrene was also studied by X‐ray crystallographic means; the molecule crystallized with two molecules in the asymmetric unit P21/n, a = 20.712(3), b = 7.8109(13), c = 13.720(2)Å, β = 107.880(11)°, Z = 8, the data refined to a final R = 0.051 for 3061 reflections. Dihedral angles between the planes of the phenyl rings were 135.00(13) and 132.52(13)° for the two independent molecules contained in the crystal. Close nonbonded S ⃛O intramolecular contacts were observed in both molecules between the sulfur and nitro‐group oxygens. Both nitro groups are twisted out of the plane of the pyridine ring and are oriented at angles of 28.75 and 38.82° respectively.
Synthesis, 13C NMR spectrum and crystal structure of 10‐Phenylpyrido[3,2‐b][1,4]benzothiazine 5‐Oxide
Authors: Jovanovic Misa V. , Biehl Edward R. , De Meester Patrice , Chu Shirley S. C. 
Published: March 2009

AbstractThe compound 10‐phenylpyrido[3,2‐b][1,4]benzothiazine 5‐oxide, 1, has been obtained in nearly quantitative yield oxidation of 10‐phenylpyrido[3,2‐b][1,4]benzothiazine with oxygen in dioxane solution. The 13C nmr chemical shift assignments of 1 are reported. Its structure has been determined by X‐ray single crystal methods. The crystals of 1 are monoclinic, space group P21/n. There are four molecules in a unit‐cell of dimensions a = 12.347(3), b = 12.947(3), c = 8.987(1)Å, β = 106.73(1)° and V = 1375.8(5) Å3. The central ring is in a boat conformation and the sulfoxide oxygen atom occupies the axial position. The folding angle between the planes of the pyrido and the benzo planes is 161.55(9)°.
Addition de la proline à quelques alcènes et alcynes électrophiles
Authors: Yebdri Okacha , Texier Fernand 
Published: March 2009

AbstractL'addition de la proline aux esters propiolique et phényl propiolique dans l'anhydride acétique conduit aux pyrroles isomères 5 et 6.L'addition de la proline dans les mêmes conditions opératoires aux alcènes électrophiles pY‐PhCH = C(X) (CN) conduit à une pyrroline‐2 8 qui élimine HCN pour conduire au pyrrole 9. L'addition de la proline au fumarodinitrile est particulière, la réaction conduit à un mélange d'acide α‐aminé 10 et de composé 11. La structure de ce compose 11 est confirmée par diffraction RX.
Preparation of [23]cyclophane‐1,2‐diones by the reaction of 3,6;12,15‐Di‐1,4‐benzo[6.6](3,4)‐1,2,5‐thiadiazolocyclophanes with grignard reagents
Authors: Hatta Taizo , Mataka Shuntaro , Tashiro Masashi 
Published: March 2009

Abstract3,6;12,15‐Di‐1,4‐benzo[6.6](3,4)‐1,2,5‐thiadiazolocyclophanes 1a‐c were prepared starting from 3,4‐di‐p‐tolyl‐1,2,5‐thiadiazole 3 and converted into [23]cyclophane‐1,2‐diones 2a‐c by the reaction with Grignard reagents.
Nucleophilic displacements of N‐aryl and heteroaryl groups. Part 8 . Intermolecular reactions of N‐aryl‐pyridinium, ‐quinolinium, and ‐acridinium salts with nucleophiles
Authors: Katritzky Alan R. , Wittmann Dieter K. , Chen Jen‐Luan , Marson Charles M. , Ossana Andrea 
Published: March 2009

AbstractN‐Aryl‐mono‐, ‐tri‐ and ‐pentacyclic pyridinium cations react with S‐ and C‐nucleophiles to give: (i) simple addition of hydride at the α‐ring position, (ii) nucleophilic addition of thiophenoxide at the γ‐ring position, (iii) deprotonation at the 6‐position of a 5,6‐dihydroquinolinium ring followed by prototropic shift to give a 1,2‐dihydroquinoline derivative, (iv) ring contraction of a pyridine to a pyrrole ring, and (v) nucleophilic displacement of the N‐aryl group.
Synthesis of 6H,8H‐isoquino[2,3‐c][1,3]benzothiazin‐8‐ones
Authors: Fodor Lajos , Szabó János , Bernáth Gábor , Sohár Pál , Maclean David B. , Smith Richard W. , Ninomiya Ichiya , Naito Takeaki 
Published: March 2009

Abstract6H,8H‐Isoquino‐1,3‐benzothiazin‐8‐ones have been prepared by reaction of 6,7‐dimethoxy‐2H‐1,3‐benzo‐thiazines with homophthalic anhydride and by photocyclization of 3‐benzoyl‐4‐methylene‐6,7‐dimethoxy 2H‐1,3‐benzothiazine. The compounds are thia analogues of protoberberine alkaloids containing a sulfur atom at C‐5 and a lactam function at C‐8. The mass spectra of the title compounds are discussed.
The syntheses of 4b,5a‐dihydro‐5H‐benzo[3,4]‐phenanthro[1,2‐b]azirine and 1a,11b‐dihydro‐6,11‐dimethyl‐1H‐benz[3,4]anthra[1,2‐b]azirine
Authors: Abu‐Shqara Elias , Blum Jochanan 
Published: March 2009

AbstractThe syntheses of the K‐imine derivatives of carcinogenic benzo[c]phenanthrene and 7,12‐dimethylbenz‐[a]anthracene are described. Treatment of trans‐5‐azido‐5,6‐dihydrobenzo[c]phenanthren‐6‐ol (3) and trans‐6‐azido‐5,6‐dihydrobenzo[c]phenanthren‐5‐ol (5) with thionyl chloride yielded the corresponding β‐chloro azides, which in turn, were reacted with lithium aluminium hydride to give 4b,5a‐dihydro‐5H‐benzo[3,4]‐phenanthro[1,2‐b]azirine (2). In a similar manner trans‐5‐azido‐5,6‐dihydro‐7,12‐dimethylbenz[a]anthracen‐6‐ol (11) and trans‐6‐azido‐5,6‐dihydro‐7,12‐dimethylbenz[a]anthracen‐5‐ol (13) were transformed to the respective chloro azides and, converted into 1a,11b‐dihydro‐6,11‐dimethyl‐1H‐benz[3,4]anthra[1,2‐b]azirine (10).
Synthesis of 1‐trifluoroacetyl‐3‐dialkylamino‐methyl‐5‐monosubstituted benzimidazoline‐2‐thiones using trifluoroacetic acid as an acylating agent
Authors: Joshi Krishna C. , Misra Ram A. , Jain Renuka , Sharma Kanti 
Published: March 2009

Abstract1‐Trifluoroacetyl‐3‐dialkylaminomethyl‐5‐monosubstituted benzimidazoline‐2‐thiones have been synthesized from p‐substituted anilines which were acetylated with trifluoroacetic acid. The trifluoroacetanilides were nitrated, reduced and cyclised with carbon disulphide in the presence of alcoholic potassium hydroxide and finally treated with formaldehyde and suitable secondary amines to afford the Mannich bases. The compounds were characterised by their analytical and spectral (ir, pmr, 19F and mass) data. The synthesized compounds have been screened for anti‐inflammatory and analgesic activity and found to be active.
Investigation of the reactions of fluorine containing 3‐hydrazino‐5H‐1, 2, 4‐triazino[5, 6‐b]indoles with ethyl acetoacetate. Synthesis of some novel tetracyclic ring systems
Authors: Joshi Krishna C. , Dandia Anshu , Baweja Sunita 
Published: March 2009

AbstractNovel tetracyclic ring systems viz. 3‐methyl‐1‐oxo‐12H‐1, 2, 4‐triazepino[3′,4′:3, 4][1, 2, 4]triazino[5, 6‐b]indole (4a) and 3‐methyl‐5‐oxo‐12H‐1, 2, 4‐triazepino[4′,3′:2, 3][1, 2, 4]triazino[5, 6‐b]indole (5a), having angular and linear structures respectively, were synthesized by the cyclization of 3‐oxobutanoic acid [5H‐1, 2, 4‐triazino‐[5, 6‐b]indole‐3‐yl]hydrazone (3a). However, cyclization of 3b (R = CHa, R1 = R2 = H) afforded the angular product 4b exclusively. Moreover, cyclization of 3c (R = R3 = H, R1 = F) yielded 7‐fluoro‐1‐0xo‐10H‐1, 3‐imidazo[2′,3′:3, 4][1, 2, 4]triazino[5, 6‐b]indole (6c) and 7‐fluoro‐3‐oxo‐10H‐1, 3‐imidazo[3′,2′:2, 3][1, 2, 4]triazino‐[5, 6‐b]indole (7c) instead of the expected triazepinone derivatives. Compound 3d (R = R1 = H, R2 = CF3) also gave an imidazole derivative but only one angular product was obtained. In all these reactions, formation of the angular product involving cyclization at N‐4 is favoured. Characterization of these products have been done by elemental analyses, ir, pmr, 19F nmr and mass spectral studies.
Site‐and regioselective π4S + π2S cycloaddition of nitrileoxides to pyridazin‐3‐ones: Formation of novel 3a, 7a‐dihydroisoxazolo[4, 5‐d]pyridazin‐4‐ones
Authors: Srinivasan T. N. , Sattur P. B. , Rao K. Rama , Prasad A. S. Bhanu , Jemmis E. D. 
Published: March 2009

AbstractA study of the cycloaddition behaviour of substituted pyridazin‐3‐ones with arylnitrile oxides has been carried out, Nitrile oxides udergo site and regioselective 1, 3‐dipolar cycloaddition to 4, 5‐double bond of pyridazinone to afford 3a, 7a‐dihydroisoxazolo[4, 5‐d]pyridazin‐4‐ones. The reactions follow frontier orbital predictions. Nitrile oxide HOMO‐pyridazinone LUMO combination is dominant.
Synthèse de 5H‐isoquino[6, 7‐b][1, 6]naphtyridones‐12 substituées sur leur sommet 10
Authors: Rivalle Christian , Huel Christiane , Bisagni Emile 
Published: March 2009

AbstractDeux chloro‐10‐5H‐isoquino[6, 7‐b][1, 6]naphtyridones‐12 ont été synthétisées au départ d'acides chloro‐4 nicotiniques et de l'amino‐6 méthyl‐5 2H‐isoquinolone‐1, cyclisation des acides intermédiaires par l'acide sul‐furique ou l'acide trifluorométhanesulfonique puis chloration par l'oxychlorure de phosphore.La comparaison de la cytotoxicité des diéthylamino‐propylamino‐10 méthyl‐6‐H‐isoquino[6, 7‐b][1, 6]naphtyridones‐12‐obtenues par substitution des dérives chlorés‐ avec celle des aza‐9 ellipticines qui leur sont appar‐entées, montre que le remplacement du noyau pyrrole par un cycle pyridone‐4 entralne une perte d'activité biologique.
Hantzsch reaction of 3‐(2‐bromoacetyl)tropolone. Synthesis of 3‐(4‐thiazolyl)tropolones
Authors: Qian Chang‐Yi , Jin Zhong‐Tian , Yin Bing‐Zhu , Imafuku Kimiaki 
Published: March 2009

Abstract3‐Acetyltropolone was brominated with phenyltrimethylammonium tribromide to afford 3‐(2‐bromoacetyl)‐tropolone (2), whose reactions with thiourea, thioformamide, and ammonium dithiocarbamate gave respectively 3‐(2‐amino‐4‐thiazolyl)‐, 3‐(4‐thiazolyl)‐, and 3‐(2‐mercapto‐4‐thiazolyl)tropolone. In a similar manner, compound 2 was treated with six 1‐substituted 2‐thioureas and three thioamides to give the corresponding 3‐(4‐thiazolyl)tropolone derivatives.
Carbamates, thiolcarbamates, dithiocarbamates and thioncarbamates derived from 2‐benzothiazolinone and benzoxazolinone
Authors: D'Amico John J. , Bellinger Frederic G. 
Published: March 2009

AbstractThe reaction of 3‐(2‐hydroxyethyl)‐2‐benzothiazoline with methyl, phenyl isocyanate, or dimethylcarbamoyl chloride afforded the carbamates 1–4. The carbanilate 5 was prepared by the reaction of 2‐benzothiazolinone with 3‐chloropropyl‐N‐methylcarbanilate under basic conditions. The reaction of the appropriate 2‐benzothiazolinone with the appropriate 2‐chloro or 3‐chloropropyl disubstituted thiolcarbamate under basic conditions furnished the thiolcarbamates 6–14. The thiolcarbamate 15 was prepared by the reaction of sodium di‐isopropylthiolcarbamate with 3‐(chloromethyl)‐2‐benzothiazolinone. The reaction of 3‐(chloromethyl)‐2‐ben‐zothiazolinone and related compound with the appropriate sodium or triethylamine salt of disubstituted dithiocarbamate afforded the dithiocarbamate 16–22. The reaction of the appropriate xanthate with the potassium salt of bromoacetic acid and the appropriate secondary amine afforded the thionocarbamates 23–29. The thionocarbamate 30 was synthesized by the reaction of 5‐chloro‐2‐benzothiazolinone with 3‐chloropropyl diethylthionocarbamate.
A selective synthesis of novel isoxazolo[2, 3‐a]‐quinoxalines and pyrrolo[1, 2‐a]quinoxalines
Authors: Kim Ho Sik , Kurasawa Yoshihisa , Takada Atsushi 
Published: March 2009

AbstractThe isoxazolo[2, 3‐a]quinoxalines 11a, b and pyrrolo[1, 2‐a]quinoxalines 12a, b were selectively synthesized from the 2‐substituted 6‐chloroquinoxaline 4‐oxides 10a, b. The pyrrolo[1, 2‐a]quinoxalines 12a, b were clarified to be produced by the ring transformation of the isoxazolo[2, 3‐a]quinoxalines 11a, b.
The reductive repair of 1, 3‐dhnethylthymine bromohydrin into 1, 3‐dimethylthymine by 1, 5‐dihydro‐5‐deazaflavin or 1, 4‐dihydroquinoline
Authors: Akiyama Taishin , Tanaka Kiyoshi , Yoneda Fumio 
Published: March 2009

AbstractThe reductive conversion of 1, 3‐dimethylthymine bromohydrin into 1, 3‐dimethylthymine by 10‐ethyl‐3‐methyl‐1, 5‐dihydro‐5‐deazaflavin or 1‐benzyl‐3‐carbamoyl‐1, 4‐dihydroquinoline has been achieved in the presence of trifluoroacetic acid.
A versatile route to potential dihydrofolate reductase inhibitors via the hitherto unknown 6‐benzyl‐2‐(O‐methyl)uracils: Synthesis of isotrimethoprim
Authors: Botta Maurizio , Artico Marino , Massa Silvio , Gambacorta Augusto 
Published: March 2009

AbstractThe synthesis of 2, 4‐diamino‐6‐(3, 4, 5‐trimethoxybenzyl)pyrimidine (isotrimethoprim) has been accomplished starting from 2‐(O‐methyl)‐6‐(3, 4, 5‐trimethoxybenzyl)uracil by standard procedures. The benzyluracil derivative has been obtained by reacting O‐methylisourea sulphate and ethyl 3, 4, 5‐trimethoxyphenacetylace‐tate.
Synthesis and cardiotonic activity of pyrimido[5,4‐b][1,4]oxazinones and 1,4‐dioxino[2,3‐d]pyrimidines
Authors: Mátyus Péter , Makk Nándor , Tegdes Anikó , Kosáry Judit , Kasztreiner Endre , Podányi Benjamin , Rabloczky György , Kiirthy Mária 
Published: March 2009

AbstractThe new pyrimido[5,4‐b][1,4]oxazinones 4a‐c and 6a,b, 7a,c were obtained from 6‐amino‐2,3‐dimethyl‐4(3H)‐pyrimidone (1) and 4‐substituted pyrimido[5,4–6][1,4]oxazinones 5, 7a, respectively, while derivatives 8a‐e of the novel ring system 1,4‐dioxino[2,3‐d]pyrimidine were prepared starting from 2b.Compounds 4a, 4c and 7a showed positive inotropic effect.
Preparation of new macrocyclic polyamines containing 4‐(phenylethynyl)pyridine subunit
Authors: Takalo Harri , Kankare Jouko 
Published: March 2009

AbstractTwo new tetraazacycloalkane‐N‐acetic acids containing 4‐(phenylethynyl)pyridine subunit as a part of macrocycle have been prepared. Two methods for the cyclisation reaction were investigated.
Diheterocyclic compounds from dithiocarbamates and derivatives thereof. I. 2,2′‐(arylenediamino)bisbenzoazoles, 2,2′‐(arylenediamino)bis(imidazopyridines) and 8,8′‐(arylenediamino)bispurines
Authors: Garín Javier , Meléndez Enrique , Merchán Francisco L. , Merino Pedro , Orduna Jesús , Tejedor Rosa , Tejero Tomás 
Published: March 2009

AbstractA general method for the synthesis of the title compounds 5, 6, 10, 14, 15 and 16 is reported. All of them were prepared in one step from readily available dimethyl N,N'‐(arylene)bisdithiocarbamates 1 and red mercury(II) oxide. The superiority of these reagents over the corresponding diisothiocyanates 7 and the synthetic utility of tetramethyl N,N'‐(arylene)bisdithiocarbonimidates 2 are also discussed.
Syntheses and conformational analyses of some 3‐amino‐2,5‐dioxo‐2,3,4,5‐tetrahydro‐1H‐1‐benzazepine derivatives: X‐ray crystal structure of 35–3‐[[(1,1‐dimethylethoxy)carbonyl]amino]‐2,5‐dioxo‐2,3,4,5‐tetrahydro‐1H‐1‐benzazepine
Authors: Ball Jonathan B. , Wong Margaret G. , Capuano Benny , Gulbis Jacqueline M. , Mackay Maureen F. , Alewood Paul F. 
Published: March 2009

AbstractThe constrained dipeptide mimic 1 was synthesized from 2 in three steps with 65% overall yield. Analyses of the 1H nmr data of a number of 3‐amino‐2,5‐dioxo‐2,3,4,5‐tetrahydro‐1H‐1‐benzazepine derivatives led to the conclusion that these compounds adopt a similar conformation and that this ring system is rigid. X‐ray crystallography was used to define the structure of 3, and computer‐aided energy minimization of 6 gave a preferred conformation similar to that observed in the crystal of 3.
Reaction of 2‐dimethylaminomethylene‐1,3‐diones with dinucleophiles. VIII. Synthesis of ethyl and methyl 2,4‐disubstituted 5‐pyrimidinecarboxylates
Authors: Schenone Pietro , Sansebastiano Laura , Mosti Luisa 
Published: March 2009

AbstractReaction of ethyl or methyl 2‐dimethylaminomethylene‐3‐oxoalkanoates with N‐C‐N dinucleophiles such as guanidine, acetamidine or benzamidine afforded in high yields the relative esters of 4‐substituted 2‐amino‐, 2‐methyl‐ or 2‐phenyl‐5‐pyrimidinecarboxylic acids, respectively. These esters were hydrolyzed to the corresponding carboxylic acids, which were converted by heating to 4‐substituted 2‐pyrimidinamines, 2‐methyl or 2‐phenylpyrimidines, respectively, generally in excellent yields. The 4‐unsubstituted ethyl 2‐amino‐, 2‐methyl‐ and 2‐phenyl‐5‐pyrimidinecarboxylates were obtained in moderate yields by reaction of the above dinucleophiles with ethyl 2,2‐diformylacetate. These esters were hydrolyzed and the corresponding acids (with the exception of the 2‐methyl derivative) were decarboxylated to give 2‐pyrimidinamine and 2‐phenylpyrimidine in satisfactory yields.
Theoretical reaction indices for dibenz[a,h]acridine
Authors: Soriano David S. , Draeger Jon A. 
Published: March 2009

AbstractHuckel molecular orbital calculations and application of Seybold‐Smith reactivity theory suggest that the Bay‐Region diol epoxide derived from the 8,9,10,11‐benzo ring of dibenz[a,h]acridine (1) is the same in reactivity as that of the 1,2,3,4‐ring in agreement with experimental findings. The calculations dispute an earlier claim of regioselective reactivity at the 8,9,10,11‐benzo ring.
Reactivity of 4‐amino‐6,7‐diphenyl‐8H‐pyrazino[2,3‐c]‐1,2,6‐thiadiazine 2,2‐dioxide towards methylating agents
Authors: Goya Pilar , Páez Juan Antonio , Pfleiderer Wolfgang 
Published: March 2009

AbstractReaction of the title compound with different methylating agents to give mono‐, di‐ and trisubstituted derivatives has been studied.
Synthesis of isoxazolo[4,5‐d]pyridazin‐4(5H)‐ones and 4‐acyl‐5‐hydroxy‐3(2H)‐pyridazinones
Authors: Chantegrel Bernard , Deshayes Christian , Pujol Bernard , Wei Zhong Jia 
Published: March 2009

AbstractThe title compounds were prepared from ethyl 5‐acyl‐ or 5‐(1‐hydroxyethenyl)isoxazole‐4‐carboxylates which in turn were prepared from ethyl 3‐methylamino‐2‐butenoate or 3(2H)‐furanones.
The synthesis of benzofuroquinolines. VII. Some benzo[h]benzofuro[2,3‐b]‐ and [3,2‐c]quinoline derivatives
Authors: Yamaguchi Seiji , Yoshimoto Yoshiteru , Murai Rikuko , Ohama Eiko , Kawase Yoshiyuki 
Published: March 2009

AbstractBenzo[h]benzofuro[3,2‐c]quinoline (2a) and its 6‐methyl derivative 2b were synthesized by the demethyl‐cyclization of 3‐(o‐methoxyphenyl)‐4(H)‐benzo[h]quinolinone (5a) and its 2‐methyl derivative 5b. And, two benzo[h]benzofuro[2,3‐b]‐ and [3,2‐c]quinolinones 8 and 9 were synthesized by the demethyl‐cyclization of 4‐hydroxy‐3‐(o‐methoxyphenyl)‐2(1H)‐benzo[h]quinolinone (7), and they were converted to the corresponding chloro derivatives 1c and 2c and benzo[h]benzofuro[2,3‐b]quinoline‐7‐carbonitrile (1d).
Synthetic routes to 2‐(2‐benzofuranyl)benzoic acids and their cyclization into benz[6]indeno[2,1‐d]furan‐10‐ones
Authors: Guillaumel Jean , Boccara Nicole , Demerseman Pierre 
Published: March 2009

AbstractThe benz[6]indeno[2,1‐d]furan‐10‐ones 1 were prepared by the intramolecular cyclization of the 2‐(2‐benzofuranyl)benzoic acids, 2, the unequivocal routes to which are described herein. Various synthetic methods to these acids were tested, as well as the methods to cyclize them.
N‐Amination of 3‐amino‐1,2,4‐triazole with hydroxylamine‐O‐sulfonic acid: Synthesis of 1,5‐diamino‐1,2,4‐triazole
Authors: Salazar Loreto , Espada Modesta , Avendaño Carmen , Elguero José 
Published: March 2009

AbstractN‐Amination of the 3(5)‐amino‐1,2,4‐triazolide anion with hydroxylamine‐O‐sulfonic acid is studied. This method provided an access to the previously unknown 1,5‐diamino‐1,2,4‐triazole.
Carbazoledioxazines having long alkyl groups 1. Synthesis of carbazoledioxazines with linear type structure
Authors: Ikeda Masaaki , Kitahara Kiyoshi , Nishi Hisao , Kozawa Kozo , Uchida Tokiko 
Published: March 2009

AbstractCarbazoledioxazines with linear type structure (5,15‐dialkyl‐8,18‐dichloro‐5,15‐dihydrodiindolo[3,2‐b:‐3′,2′‐m]triphenodioxazine) were selectively synthesized by demethanolation ring closure of 2,5‐bis(2‐methoxy‐9‐alkyl‐3‐carbazolylamino)‐3,6‐dichloro‐1,4‐benzoquinone in a high boiling solvent. The structure has been confirmed by 1H‐nmr and X‐ray crystallography.