bluuebunny/crossref_metadata_2025_split huggingface dataset:
7‐Deaza‐5′‐noraristeromycin derivatives resembling L‐toyocamycin and L‐sangivamycin
Authors: Seley Katherine L. , Schneller Stewart W. 
Published: March 2009

AbstractThe synthesis of the 7‐cyano and 7‐carboxamido derivatives of 7‐deaza‐5′‐noraristeromycin have been prepared in 3 and 4 steps, respectively, for evaluation as anti‐trypanosomal agents. Neither compound was active in the latter assay.
Palladium‐catalyzed synthesis of 3‐oxo‐1,3‐dihydro‐1‐isobenzofuranyl alkanoates from 2‐bromobenzaldehyde and sodium alkanoates
Authors: Cho Chan Sik , Baek Dong Yeol , Shim Sang Chul 
Published: March 2009

Abstract2‐Bromobenzaldehyde reacts with sodium alkanoates in acetonitrile under carbon monoxide pressure in the presence of a catalytic amount of bis(triphenylphosphine)palladium(II) chloride to afford the corre sponding 3‐oxo‐1,3‐dihydro‐1‐isobenzofuranyl alkanoates in moderate to good yields.
A slightly shorter route to carbocyclic nucleosides. Synthesis of (±)‐trans‐1‐[2‐(hydroxymethyl)cyclopentylmethyl]uracil
Authors: Santana Lourdes , Teijeira Marta , Uriarte Eugenio 
Published: March 2009

Abstract(±)‐trans‐1‐[2‐(Hydroxymethyl)cyclopentylmethyl]uracil (1) was prepared in two steps and 56% yield from 2‐hydroxymethylcyclopentylmethylamine (7) and 3‐methoxy‐2‐propenoylisocyanate (6). Isocyanate 6 was prepared from methyl 3‐methoxy‐2‐propenoate in four steps and 38% overall yield.
Synthesis of spiroisoindolinones by palladium‐catalyzed heterocyclization of 2‐iodobenzoyl chloride with ketimines
Authors: Cho Chan Sik , Wu Xue , Jiang Li Hong , Shim Sang Chul , Kim Hong Rak 
Published: March 2009

Abstract2‐Iodobenzoyl chloride reacts with ketimines in acetonitrile at 100° under carbon monoxide pressure in the presence of a catalytic amount of a palladium catalyst together with triethylamine to afford the corresponding spiroisoindolinones in high yields.
Unusual dihydrazone formation in the fischer‐indole cyclization. The synthesis of novel nonclassical annulated 2,4‐Diamino‐pyrrolo[2,3‐d]pyrimidine antifolates
Authors: Gangjee Aleem , Chen Lihua 
Published: March 2009

AbstractThe synthesis of seven novel tetracyclic 2,4‐diaminopyrrolo[2,3‐d]pyrimidines as conformationally restricted nonclassical antifolates was achieved via an unusual Fischer‐indole cyclization of dihydrazones. An attempted synthesis of 2,4‐diamino‐6‐hydrazinopyrimidine afforded 2‐amino‐4,6‐dihydrazinopyrimidine which when reacted with appropriate ketones gave the dihydrazones. The dihydrazones in turn under Fischer‐indole cyclization conditions afforded target conformationally restricted tetracyclic products.
Exploratory chemistry of 3‐aroylformamido‐4‐aryl‐1,2,5‐thiadiazoles
Authors: Kong Yung Cheol , Kim Kyongtae 
Published: March 2009

AbstractApart from the previous report, the reaction of 3‐(4‐nitrobenzoylformamido)‐4‐(4‐nitrophenyl)‐1,2,5‐thiadiazole (2a) with m‐chloroperbenzoic acid in chloroform at room temperature did not proceed, whereas at reflux temperature the same reaction gave 4‐nitrobenzoic acid (5) (86%) and a minute amount of a mixture of 4‐nitrobenzoylformamide (6) and 3‐amino‐4‐(4‐nitrophenyl)‐1,2,5‐thiadiazole (7a). On the other hand the same reaction in a mixture of ethanol and chloroform (1:4) at room temperature gave 3‐ethoxycarbamoyl‐4‐(4‐nitrophenyl)‐1,2,5‐thiadiazole (8a) (24%) as an isolable product. When 3‐aroylformamido‐4‐aryl‐1,2,5‐thiadiazoles 2 in tetrahydrofuran were treated with various alkoxides in the corresponding alcohols at room temperature, 3‐amino‐4‐aryl‐ 7, 3‐alkoxycarbamoyl‐4‐aryl‐ 8, and 3‐aryl‐4‐(aryl)(hydroxy)acetamido‐1,2,5‐thiadiazoles 9 were isolated. The ratios of which were dependent on the kind of bases and the solvent employed. Selected compounds 2 were allowed to react with phosphorus pentasulfide in the presence of pyridine at reflux to give 3‐aryl‐4‐arylacetarnido‐1,2,5‐thiadiazoles 17 (55–64%), which were also produced by the reaction of 2 with either Lawesson's reagent or hydrogen sulfide gas in the presence of pyridine at reflux.
A Comparison of the hyphenated experiments GHMQC‐TOCSY and GHSQC‐TOCSY
Authors: Hadden Chad E. , Martin Gary E. , Luo J.‐K. , Castle Raymond N. 
Published: March 2009

AbstractHeteronuclear shift correlations generally may be established using either the multiple quantum‐based GHMQC experiment or, alternately, the single quantum‐based GHSQC experiment. A scant few reports contained in the literature have compared results obtained with both types of sequences. The F1 resolution of the GHMQC and GHSQC experiments are compared using the polynuclear heteroaromatic naphtho‐[2′,1′:5,6]naphtho[2′,1′:4,5]thieno[2,3‐c]quinoline. Even when augmented by linear prediction in F1, the single quantum‐based GHSQC sequence gives better F1 resolution than its multiple quantum counterpart. To date, no studies have compared the hyphenated analogs of these experiments, GHMQC‐ and GHSQC‐ TOCSY. Similar conclusions to GHMQC/GHSQC are drawn for the comparison of GHMQC‐ and GHSQC‐ TOCSY experiments with inverted direct responses with, and without, linear prediction. The latter is recommended whenever there is congestion in both the F2 and F1 frequency domains.
Reductive cyclization of carbohydrate 2‐nitrophenylhydrazones to chiral functionalized 1,2,4‐benzotriazines and benzimidazoles
Authors: Andersch Jens , Sicker Dieter 
Published: March 2009

AbstractThe 2‐nitrophenylhydrazones 2 of D‐arabino‐2‐hexulopyranosonic acid, D‐arabinose, D‐galactose and D‐galacturonic acid are used as precursors to form chiral functionalized 1,2,4‐benzotriazines and benzimidazoles by reductive cyclization methods. Catalytic hydrogenation provided the amine derivatives which are cyclized and air oxidized in alkaline solution to yield the novel 1,2,4‐benzotriazines 3 as the main products, while on acid catalysis the benzimidazoles 4 are formed.
An alternative synthesis of piritrexim, a lipophilic inhibitor of human dihydrofolate‐reductase
Authors: Troschütz Reinhard , Zink Mario , Gnibl Rainer 
Published: March 2009

AbstractAn alternative synthesis of the lipophilic antifolate piritrexim (1) is outlined. Starting from ketone 2, treatment with phosphorus oxychloride and dimethylformamide gave the β‐chlorocrotonaldehydes 3E/Z, which were reacted with cyanoacetamide (6) in the presence of sodium hydride to yield a 3‐cyano‐2‐pyridone derivative 7. Chlorination of 7 with thionyl chloride and subsequent reaction with guanidine (9) gave rise to piritrexim (1). The reaction of β‐chlorocrotonaldehydes 3E/Z, with 2,4,6‐triaminopyrimidine (4) yielded iso‐piritrexim (5).
One‐step synthesis of novel 2,4‐diaminopyrimidine antifolates from bridged alicyclic ketones and cyanoguanidine
Authors: Rosowsky Andre , Papoulis Andrew T. , Queener Sherry F. 
Published: March 2009

AbstractA convenient one‐step reaction with cyanoguanidine was used to convert alicyclic ketones to previously undescribed 2,4‐diamino‐5,6,7,8‐tetrahydroquinazolines with a one‐, two‐, or three‐carbon bridge in the carbocyclic ring. Although the yields of the desired products were modest, the principal advantage of this one‐step process was that it provided easy access to a variety of novel bridged heterocyclic ring systems whose synthesis from sterically hindered ketones by other methods would have required multiple steps with an even lower overall yield. The products were tested as inhibitors of dihydrofolate reductases from Pneumocystis carinii, Toxoplasma gondii, and rat liver with a view to examining the effect of a space‐filling bridge on binding. The most potent and selective compound in the group was 4,6‐diamino‐3,5‐diazatricyclo[7.2.1.02,7]dodeca‐2,4,6‐triene (13), whose potency and selectivity approached those of trimethoprim, a drug commonly used to treat P. carinii and T. gondii infection. 3,5‐Diamino‐4,6‐diazatricyclo[6.2.1.02,7]‐undeca‐2,4,6‐triene (14), the analog of 13 with a one‐carbon rather than a two‐carbon bridge showed similar potency and selectivity against the T. gondii enzyme, but was a weak and nonselective inhibitor of P. carinii dihydrofolate reductase. The other compounds tested were likewise weak and nonselective.
Ring transformation of 3‐halo‐4‐methoxycoumarins into pyrazoles with hydrazines
Authors: Morita Hikari , Harada Kazuho , Okamoto Yoshihisa , Takagi Kaname 
Published: March 2009

Abstract3‐Chloro‐ and 3‐bromo‐4‐methoxycoumarins 1a,b were readily transformed into 4‐halo‐5‐(2‐hydroxyphenyl)‐3‐oxo‐2,3‐dihydropyrazoles 2a,b with hydrazines. In the reaction of 1a,b with excess hydrazine and phenylhydrazine in boiling ethanol, unexpected 4‐hydrazono‐3‐(2‐hydroxyphenyl)‐2‐pyrazolin‐5‐ones 3, 5 were obtained. The structure of 3 was determined by X‐ray diffraction analysis.
Syntheses of diaza‐18‐crown‐6 ligands containing two units each of 4‐hydroxyazobenzene, benzimidazole, uracil, anthraquinone, or ferrocene groups
Authors: Su Ning , Bradshaw Jerald S. , Zhang Xian X. , Savage Paul B. , Krakowiak Krzysztof E. , Izatt Reed M. 
Published: March 2009

AbstractSix new diaza‐18‐crown‐6 ligands each containing two aromatic side arms with responsive functions were prepared. Diaza‐18‐crown‐6 containing two 4‐hydroxyazobenzene (3) or two 4‐hydroxy‐4′‐(dimethyl‐amino)azobenzene (4) substituents were prepared via a one‐pot Mannich reaction. Diaza‐18‐crown‐6 containing two benzimidazole (5), two uracil (6) or two 9,10‐anthraquinone (7) substituents were prepared by treating the diazacrown with the appropriate chloromethyl‐containing compound. Reductive amination using sodium triacetoxyborohydride, diaza‐18‐crown‐6 and ferrocenecarboxaldehyde was used to prepare bisferrocene‐substituted diaza‐18‐crown‐6 (8). Interactions of compounds 3, 5, and 6 with Na+, K+, Ba2+, Ag+, and Cu2+ were evaluated by a calorimetric titration technique at 25° in methanol. All three ligands form more stable complexes with Ag+ and Cu2+ (5 forms a precipitate with Ag+) than with Na+ and K+. Ligand 5 also forms a highly stable complex with Ba2+.
An efficient general synthesis of 1‐(benzotriazol‐1‐yl)alkyl esters
Authors: Katritzky Alan R. , Pastor Alfredo , Voronkov Michael V. 
Published: March 2009

Abstract1‐(Benzotriazol‐1‐yl)alkyl esters 2a‐u were obtained in yields averaging 86% by the direct reaction of various aldehydes with the corresponding N‐acylbenzotriazoles in the presence of a catalytic amount of potassium carbonate (10–25 mole %). The procedure was optimized by evaluating the effects of solvent, catalyst, temperature and other parameters.
Oxidative ring‐opening of rel‐(2R,3R,5S)‐5‐aryl‐2‐benzoylamino‐6,7‐bis(methoxycarbonyl)‐2,3‐dihydro‐1‐oxo‐3‐phenyl‐1H,5H‐pyrazolo[1,2‐a]‐pyrazoles. Synthesis of rel‐(2R,3R)‐3‐phenyl‐3‐[5‐aryl‐3,4‐bis(methoxycarbonyl)pyrazolyl‐1]alanine esters
Authors: Prešeren Andrej , Svete Jurij , Stanovnik Branko 
Published: March 2009

Abstractrel‐(2R,3R)‐N‐Benzoylamino‐6,7‐bis(methoxycarbonyl)‐2,3‐dihydro‐1‐oxo‐1H,5H‐pyrazolot[1,2‐a]‐pyrazoles 5, accesible by cycloaddition of dimethyl acetylenedicarboxylate (3) to (1Z)‐rel‐(4R,5R)‐1‐aryl‐methylidene‐4‐benzoylamino‐5‐phenyl‐3‐pyrazolidinone‐1‐azomethine imines 4, undergo oxidative ring cleavage with methanolic bromine giving rel‐(2R,3R)‐N‐benzoyl‐3‐phenyl‐3‐[5‐aryl‐3,4‐bis(methoxy‐carbonyl)pyrazolyl‐1]alanine methyl esters 6 as products.
Synthesis of polyazacyclophane‐intercalator conjugates for combinatorial chemistry and RNA interaction studies
Authors: Wang Tingmin , An Haoyun , Haly Becky D. , Dan Cook P. 
Published: March 2009

AbstractAnthraquinone and pyrene intercalators were conjugated to different positions of several polyaza‐pyridinocyclophanes by various linkers to provide thirteen new polyazacyclophane‐intercalator conjugates 1–13. These resulting conjugates contain two or three constrained secondary nitrogen atoms on the ring, which may serve as nucleophilic, coordinating or hydrogen‐bonding sites for combinatorial, RNA interaction and coordination studies.
Synthesis of 1,2‐oxazaheterocycles containing an isoindolone moiety from N‐Hydroxyphthalimide
Authors: Bartovic Alexander , Decroix Bernard , Netchitaïlo P. 
Published: March 2009

AbstractSyntheses of the isoindolobenzoxazinone 1a and thienoxazinoisoindolones 1b,c was developed from N‐hydroxyphthalimide 3 and halogenomethylaryl derivatives. The resulting aryloxy phthalimides 4a‐c were reduced to hydroxylactams 5a‐c which cyclized in acidic conditions. A Wittig reaction on 5a using carbethoxymethylidenetriphenylphosphorane gave the corresponding acid 6 which treated in Friedel and Crafts conditions led to the isoxazolinone 8 by cleavage of the benzyl CO bond.
Lipase‐catalysed kinetic resolution of hydroxymethylchromanes
Authors: Czompa A. , Kovács T. , Antus S. 
Published: March 2009

AbstractAn effective kinetic resolution of hydroxymethylchromanes racemic 2a and 3a has been achieved by means of enantioselective transesterification with vinyl acetate in organic solvents. The alcohols (‐)‐R‐2a and (‐)‐S‐3a were obtained with high optical purities (94 and 98% ee) in 70% and 38% yields, respectively. The influence of the enzyme source and the character of the solvent on the enantioselectivity were studied.
Synthesis of novel, nonclassical 2‐amino‐4‐oxo‐6‐(arylthio)ethylpyrrolo[2,3‐d] pyrimidines as potential inhibitors of thymidylate synthase
Authors: Gangjee Aleem , Dubash Nauzer P. , Kisliuk Roy L. 
Published: March 2009

AbstractA novel series of 14 nonclassical 6‐substituted pyrrolo[2,3‐d]pyrimidines 2a ‐ 2n were designed as potential inhibitors of thymidylate synthase, based on previously reported 2‐amino‐4‐oxopyrrolo[2,3‐d]‐pyrimidines 1a and 1b. The synthesis of the target compounds 2a‐2n was accomplished by nucleophilic displacement of the mesylate 11 with appropriately substituted aromatic thiols. Most of the target compounds did not show inhibition of either Escherichia coli thymidylate synthase or recombinant human thymidylate synthase at the concentrations tested. However, compounds 2h (2,4‐dichloro), 2j (3,4‐dichloro) and 2m (4‐nitro) did show 25%, 40% and 35% inhibition of human thymidylate synthase at 23 μM, 23 μM and 24 μM, respectively. These observations are in accordance with previous reports, which suggest that strong electron withdrawing substituents on the side chain aromatic ring are conducive to inhibition of thymidylate synthase.
Design and synthesis of a novel intercalating isoxazolyl bis‐lexitropsin conjugate
Authors: Han Xiaochun , Natale Nicholas R. 
Published: March 2009

Abstract9‐Anthracene nitrile oxide directly generated from 9‐anthracenealdoxime and N‐chlorosuccinamide (NCS), reacts with dimethyl acetylenedicarboxylate (DMAD) and affords the corresponding 3‐(9′‐anthra‐cenyl)‐isoxazole‐4,5‐dicarboxylic acid ester (3) with good yield in a very short period. Double activation reaction between (3) and hydrogenated lexitropsin (5) in a 1:2 molar ratio, produced a bis‐lexitropsin product (6) (major product) and mono‐lexitropsin product (7).
Pyridopyrimidines. X. Synthesis of 3‐Substituted 2‐Thioxo‐5,7‐dimethylpyrido[2,3‐d] pyrimidin‐4(3H)‐ones and their S‐Alkylation Under Phase Transfer Conditions
Authors: Dave Chaitanya G. , Patel Killol J. 
Published: March 2009

Abstract2‐Thioxo‐5,7‐dimethylpyrido[2,3‐d]pyrimidin‐4(3H)‐ones 3 were synthesized by the cyclocondensation of 2‐amino‐3‐carbethoxy‐4,6‐dimethylpyridine 1 with methyl‐N‐aryldithiocarbamates 2 and compared with the condensation between 1 and aryl isothiocyanates 4. When a comparative study of N vs S alkylation of ambident 2‐thioxo‐5,7‐dimethylpyrido[2,3‐d]pyrimidin‐4(3H)‐ones 3 was carried out under liquid‐liquid and solid‐liquid phase transfer conditions using various alkylating agents 5, the S‐alkylated products 6 were obtained exclusively and selectively.
Synthesis of substituted pyrimido[4,5‐b] and [5,4‐c]‐[1,8]naphthyridines
Authors: Plisson Christophe , Chenault Jacques 
Published: March 2009

AbstractEthyl 1‐ethyl‐7‐methyl‐4‐oxo‐1,4‐dihydro[1,8]naphthyridine‐3‐carboxylate (1), precursor of nalidixic acid, has been converted in two steps through ([1,8]naphthyridin‐3‐yl)carbonylguanidine derivatives into substituted pyrimido[4,5‐b] and [5,4‐c][1,8]naphthyridines.
Preparation of N‐(4′,6′‐difluoro‐2′‐hydroxybenzyl)‐monoaza‐15‐crown‐5 and x‐ray crystal structure of potassium thiocyanate complex: A molecular partition wall
Authors: Habata Yoichi , Akabori Sadatoshi 
Published: March 2009

AbstractArmed monoaza‐15‐crown‐5 having a 4′,6′‐difluoro‐2′‐hydroxybenzyl group as an additional binding site (2) has been prepared by the Mannich reaction of N‐methoxymethylmonoaza‐15‐crown‐5 with 3,5‐difluorophenol. The reactive site on 3,5‐difluorophenol for the Mannich reaction was predicted by an electrostatic potential calculation (density functional calculation, SVWN/DN* method). Ligand 2 is interesting, because it has two possible binding sites (phenolic OH group and fluorine atom) in the side arm. An X‐ray crystal structure of the potassium thiocyanate complex of ligand 2 revealed that the oxygen atom of the phenolic OH group binds to the potassium cation incorporated in the crown ether ring, and two water molecules are enclosed by two armed crown ethers with the crown ethers forming partition walls.
Convenient one pot synthesis of 5‐unsubstituted pyrazolo [3,4‐c]isoquinolines
Authors: Bogza Sergei L. , Malienko Anna A. , Sujkov Sergei Y U. , Perepichka Igor F. , Bogdan Natalya M. , Dulenko Vladimir I. , Kobrakov Konstantin I. , Bryce Martin R. 
Published: March 2009

AbstractThe convenient one pot synthesis of pyrazolo[3,4‐c]isoquinolines 1 from 5‐aminopyrazoles 2 and paraformaldehyde in formic or trifluoroacetic acids is described.
Photoreaction of 1H‐azepine‐2,7‐dione in alkaline solution
Authors: Fukai Yoshihisa , Miyazawa Tomoyuki , Kojoh Mahiro , Takabatake Tohru , Hasegawa Minoru 
Published: March 2009

AbstractPhotolysis of 1H‐azepine‐2,7‐dione 2 proceeded with alkali as in the photoreaction of N‐alkylimide to give 7‐hydroxy‐1H‐azepine‐2‐one 13.
Asymmetric borane reduction of ketones promoted by menthopyrazole‐zncl2 complex
Authors: Kashima Choji , Tsukamoto Yoshihiro , Miwa Yohei , Higashide Kohei 
Published: March 2009

AbstractThe enantioselective reduction of ketones was accomplished by borane in the presence of pyrazole derivatives, particularly 2‐methoxymethyl‐3‐phenyl‐1‐menthopyrazole (8). The catalysis of zinc chloride makes it possible to lower the reaction temperature below 0 °C, and to promote enantioselectivity.
Synthesis of pyrazole‐fused azepino[5,4,3‐cd]indoles
Authors: Safieh Kayed A. Abu , El‐Abadelah Mustafa M. , Zarga Musa H. Abu , Sabri Salim S. , Voelter Wolfgang , MÖssmer Cäcilia M. 
Published: March 2009

AbstractThe synthesis of some new pyrazolo[3′,4′:6,7]azepino[5,4,3‐cd] indoles (10a‐c) was achieved via regios‐elective cyclization of the respective 3‐(4‐acylaminopyrazol‐5‐yl)indoles (9a‐c) under Bischler‐Napieralski reaction conditions. The latter compounds were obtained by acylation of the corresponding 3‐(4‐aminopyra‐zol‐5‐yl)indoles (8a,b) which, in turn, were prepared by reduction of the 3‐(4‐nitropyrazol‐5‐yl)indoles precursors (7a,b). The latter synthons were accessible from the reaction of indolylzinc chlorides (5a,b) with 5‐chloro‐1,3‐dimethyl‐4‐nitropyrazole. Ms and nmr spectral data of 10a‐c are in agreement with the assigned azepino‐indole structure as determined for 10a by X‐ray crystal measurements which demonstrate that the azepine ring is almost completely planar with the indole and pyrazole rings.
Derivatives of pyrido[2,3‐b][1,4]diazepine and of the dipyrido[1,2‐a:2′,3′‐b]imidazole heterocyclic system
Authors: Savelli Francesco , Boido Alessandro , Piacente Sonia 
Published: March 2009

AbstractWith a continuing interest in heteropolycyclic systems which may show biological activities, we studied the reaction of 3‐amino‐2‐(methylamino)pyridine with diethyl 1,3‐acetonedicarboxylate in order to develop pyridodiazepinone derivatives. From the reaction mixture, we separated dipyrido[1,2‐a:2′,3′‐d]imidazole derivatives (3 and 4) besides two isomeric pyrido[2,3‐b][1,4]diazepine derivatives (5 and 6) in which the complex structural differentiation was achieved through nmr experiments and chemical evidence. Several attempts to elaborate isomers 5 and 6 have not yet given significant results.
Cycloaddition reaction of 2‐allenylindoles with diethyl acetylenedicarboxylate under thermal and high pressure conditions
Authors: Ishikura Minoru , Uchiyama Harue , Hino Ayako , Katagiri Nobuya 
Published: March 2009

AbstractThe cycloaddition reaction of 2‐allenylindoles 2 with diethyl acetylenedicarboxylate 6 was undertaken under both thermal and high pressure reaction conditions, leading to carbazole derivatives 5.
Synthesis and anti‐HIV activity of HEPT and S‐DABO‐analogues with 5‐Benzyl and 5‐Phenyl substituents
Authors: Larsen Janus S. , Aal Mohammed Taha Abdel , Pedersen Erik B. , Nielsen Claus 
Published: March 2009

Abstract6‐Benzyl‐5‐phenyluracil (4) and 5,6‐dibenzyluracil (9) were synthesised from diphenyl acetone (1) and ethyl 3‐oxo‐4‐phenylbutyrate (6), respectively. The uracils were alkylated to afford the 1‐alkoxymethyl‐uracils 5, 10 and 11. Furthermore, S‐alkylated dihydroalkoxybenzyloxopyrimidine (S‐DABO) analogues were prepared by alkylating 5,6‐dibenzyl‐2‐thiouracil (8) on sulfur to yield compounds 12a‐f. All compounds were tested for their inhibition of HIV‐1 reverse transcriptase, and moderate activity was found for 6‐benzyl‐1‐(ethoxymethyl)‐5‐phenyluracil (5).
One ‐ pot synthesis of novel sulfur and selenium heterocycles by directed ortho‐lithiation
Authors: Wright S. W. 
Published: March 2009

AbstractA procedure for the synthesis of benzo[e][1,3]thiazine‐2,4‐diones from benzamides by directed lithiation and sequential treatment with sulfur and phosgene is reported. Use of thiophosgene afforded 2‐thioxo‐2,3‐dihydro‐benzo[e][1,3] thiazin‐4‐ones. Application of this methodology to benzenesulfonamides afforded the previously unknown 1,1‐dioxo‐1,2‐dihydro‐1,4‐dithia‐2‐aza‐naphthalen‐3‐one ring system with phosgene and the 1,2‐dioxo‐2‐phenyl‐2,3‐dihydrobenzo[e][1,4,2]dithiazine‐3‐one ring system with thiophosgene. Use of selenium in place of sulfur afforded the novel analogous selenium heterocycles, however in the case of benzamides the use of selenium and phosgene afforded benzo[d]isoselenazol‐3‐ones unexpectedly.
Synthesis of new benzylpyridines as potential photochromic compoundsa
Authors: Heynderickx Arnault , Samat André , Guglielmetti Robert 
Published: March 2009

AbstractPhotoinduced proton transfer systems such as 2‐(2′,4′‐dinitrobenzyl)pyridine derivatives have been developed in an attempt to apply the compounds to variable optical transmission materials. However their fatigue resistance property is a limitation for these applications. New benzylpyridines have been synthesized and tested. 2‐(2′,4′‐Diphenylsulfonybenzyl)pyridine was found to be photochromic in the crystalline state and in ethanolic solution (λmax= 485 nm) upon UV flash photolysis.
Synthesis of dihydrolysergol analogues
Authors: Mantegani Sergio , Traquandi Gabriella , Varasi Mario 
Published: March 2009

AbstractAs a part of a search for novel biological active ergoline derivatives, the indole ring present in the ergoline skeleton (indole[4,3‐f,g]quinoline) was converted into different heterocyclic ring systems such as quinazoline 2, benzofurane 3 and benzoxazole 4. Due to the paramount importance of chirality to attain biological activity, natural dihydrolysergic acid 1 was chosen as starting material and a synthetic pathway conservative in term of chirality was followed.