Showing papers on "Bicyclic molecule published in 1985"

A convenient synthesis of 3-acylindoles via Friedel Crafts acylation of 1-(phenylsulfonyl) indole. A new route to pyridocarbazole-5, 11-quinones and ellipticine

Abstract: Application de la reaction de Friedel et Crafts d'acylation en 3 des benzenesulfonyl-1 indoles a la synthese de pyrido [3,4-b]- et -[4,3-b] carbazolequinones-5,11 (puis d'ellipticine) et de benzo [b] carbazolequinone-6,11 (acylation par l'anhydride ou le chlorure-3 et ester de methyle-4 de l'acide pyridinedicarboxylique-3,4 ou par l'anhydride phtalique)

Further insight into magnetostructural correlations in binuclear copper(II) species related to methemocyanin: x-ray crystal structure of 1,2-.mu.-nitrito complex

Abstract: Determination de la structure de [Cu 2 (L-Et)(NO 2 )] [ClO 4 ] avec HL-Et=N,N,N'N'-tetrakis-([ethyl-1 benzimidazolyl]-2) hydroxy-2 diamino-1,3 propane

Tandem radical approach to linear condensed cyclopentanoids. Total synthesis of (.+-.)-hirsutene

Abstract: Synthese a partir de la methyl-6a tetrahydro cyclopenta [b] furannone-2, avec comme etape cle la cyclisation d'un iodoalkyl alcynyl cyclopentene intermediaire

Photoinduced cyclizations of mono- and dianions of N-acyl-o-chloroanilines and N-acyl-o-chlorobenzylamines as general methods for the synthesis of oxindoles and 1,4-dihydro-3(2H)-isoquinolinones

Abstract: L'influence du rayonnement proche UV et l'effet d'inhibiteurs impliquent un mecanisme radicalaire en chaine

Solvent effects on keto-enol equilibria: tests of quantitative models

Abstract: L'etude est faite sur les systemes protomeres suivants: dimethyl-5,5 cyclohexanedione-1,3 methyl-2 cyclohexanedione-1,3, perhydro benzo [c] furannedione-1,7, acetylacetone, acetylacetate d'ethyle et anthrone-9

Palladium-mediated vicinal cleavage of allyl epoxides with retention of stereochemistry: a cis hydroxylation equivalent

Abstract: Synthese regio- et diastereoselective de cis-diols-1,2 (sous forme de carbonate) a partir de vinylepoxydes par reaction avec le dioxyde de carbone en presence de (triisopropylphosphite) 3 palladium

Synthesis and biological activity of 6-azacadeguomycin and certain 3,4,6-trisubstituted pyrazolo[3,4-d]pyrimidine ribonucleosides.

Abstract: Several 3,4,6-trisubstituted pyrazolo[3,4-d]pyrimidine ribonucleosides were prepared and tested for their biological activity. High-temperature glycosylation of 3,6-dibromoallopurinol with 1-O-acetyl-2,3,5-tri-O-benzoyl-D-ribofuranose in the presence of BF3 X OEt2, followed by ammonolysis, provided 6-amino-3-bromo-1-beta-D-ribofuranosylpyrazolo-[3,4-d]pyrimidin-4(5H)-on e. Similar glycosylation of either 3-bromo-4(5H)-oxopyrazolo [3,4-d]pyrimidin-6-yl methyl sulfoxide or 6-amino-3-bromopyrazolo [3,4-d]pyrimidin-4(5H)-one, and subsequent ammonolysis, also gave 7a. The structural assignment of 7a was on the basis of spectral studies, as well as its conversion to the reported guanosine analogue 1d. Application of this glycosylation procedure to 6-(methylthio)-4(5H)-oxopyrazolo[3,4-d]pyrimidine-3-carboxamide gave the corresponding N-1 glycosyl derivative. Dethiation and debenzoylation of 16a provided an alternate route to the recently reported 3-carbamoylallopurinol ribonucleoside thus confirming the structural assignment of 16a and the nucleosides derived therefrom. Oxidation of 16a and subsequent ammonolysis afforded 6-amino-1-beta-D-ribofuranosyl-4(5H)-oxopyrazolo[3, 4-d]pyrimidine-3-carboxamide. Alkaline treatment of 15a gave 6-azacadeguomycin. Acetylation of 15a, followed by dehydration with phosgene, provided the versatile intermediate 6-amino-1-(2,3,5-tri-O-acetyl-beta-D-ribofuranosyl)-4(5H)-oxopyrazolo [3, 4-d]pyrimidine-3-carbonitrile. Deacetylation of 19 gave 6-amino-1-beta-D-ribofuranosyl-4(5H)-oxopyrazolo[3, 4-d]pyrimidine-3-carbonitrile. Reaction of 19 with H2S gave 6-amino-1-beta-D-ribofuranosyl-4(5H)-oxopyrazolo[3, 4-d]pyrimidine-3-thiocarboxamide. All of these compounds were tested in vitro against certain viruses and tumor cells. Among these compounds, the guanosine analogues 7a and 20a showed significant activity against measles in vitro and were found to exhibit moderate antitumor activity in vitro against L1210 and P388 leukemia. 6-Azacadeguomycin and all other compounds were inactive against the viruses and tumor cells tested in vitro.

Synthesis and biological properties of (carboxyalkyl)amino-substituted bicyclic lactam inhibitors of angiotensin converting enzyme.

Abstract: Syntheses of the potent angiotensin converting enzyme inhibitor (3S)-1-(carboxymethyl)-3-[[(1S)-1-carboxy-3-phenylpropyl]amino]- 2,3,4,5-tetrahydro-1H-[1]benzazepin-2-one (4b; CGS 14831) and the related monoester prodrug (17a; CGS 14824A) are described together with preparative details for six- and eight-membered ring analogues. Inhibitory potencies and in vivo biological activity of the compounds are discussed. The data indicate that 17a has a biological profile comparable to that of enalapril.

Intramolecular [2+2] cycloadditions of ketenes and keteniminium salts to olefins

Abstract: On prepare une serie de cetones bicycliques par cycloaddition de cetenes et de sels de ceteneiminium derives d'acides aliphatiques insatures

Synthesis of derivatives of isoindole and of pyrazino[2,1-a]isoindole

Abstract: Amines were reacted with lactones 7 or with unsaturated nitro derivatives 8 to give isoindole and pyrazino[2,1-a]isoindole derivatives. The mechanisms of formation, proofs of structure, and stereoc...

4-[(Bicyclic heterocyclyl)-methyl and -hetero]-piperidines

Abstract: 4-[(Bicyclic heterocyclyl)methyl and -hetero]-piperidines having antihistaminic and serotonin-antagonistic properties which compounds are useful agents in the treatment of allergic diseases.

Studies of rutaecarpine and related quinazolinocarboline alkaloids

Abstract: Synthese de rutecarpine, de son derive dihydro-13b,14, d'euxylophoricines et d'evodiamine et de son derive dideshydro-13,13b par cyclisation de derives de l'[indolyl-3]-2' ethyl 3H-quinazolone-4 obtenus par action de tryptamine sur des benzooxazine-3,1ones-4