Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group. More particularly, the improved process is directed toward preparation of water-soluble triazole antifungal compounds are provided having the general formula wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.

Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group.

Abstract: A purine salt of the formula ##STR1## wherein Y.sub.1 is chloro, bromo, or iodo, and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from alkyl and substituted alkyl is reacted with the compound of the formulaZ.sub.1 --Xto yield the purine of the formula ##STR2## wherein x is a leaving group, and Z.sub.1 is a protected form of the carbohydrate surrogate Z.

Abstract: (1R,trans) Diprotected 3-methylene-1,2-cyclopropanedimethanol is oxidized to an optically active diol ##STR1## which is then cyclized to an orthoester ##STR2## This orthoester is then treated with a Lewis acid catalyst to give the cyclobutanone ##STR3## which is useful as an intermediate in the preparation of the antiviral agent ?1R-(1.alpha.,2.beta.,3.alpha.)!-2-amino-9-?2,3-bis(hydroxymethyl)cyclobut yl!-1,9-dihydro-6H-purin-6-one.

Abstract: A method of preparing compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof which comprises converting a compound of the formula ##STR2## where the R.sup.2 substituent contains a hydrogen atom which is more acidic than the starred (*) hydrogen atom in formula II, to the corresponding dianion of formula ##STR3## where M is a counterion preferably lithium or magnesium, using two equivalents of a base in an inert solvent such as tetrahydrofuran; then reacting compounds of formula IIA with an epoxide of formula ##STR4## to produce the compounds of formula I.

Abstract: The present invention relates to novel 7-oxabicycloheptane carboxylic acid prostaglandin analog intermediates which may be used to prepare a final anti-thrombotic, anti-vasospastic product, and to methods for preparing the same.

Abstract: A purine salt of the formula ##STR1## wherein Y.sub.1 is chloro, bromo, or iodo, and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from alkyl and substituted alkyl.

Abstract: A novel process comprises reducing a benzazepine or benzothiazepine at the 3-position in d-cis configuration by treatment with reductase-supplying microorganisms or enzymes derived therefrom. The process can be catalyzed in a single stage by growing microbial cultures or in a two-stage fermentation/transformation by resting cell-suspensions. The enzymes derived from the microorganisms can be used in free state or immobilized form. The microorganisms and enzymes catalyzes the specific reduction with 90 to 99% conversion efficiency to 99% or greater optical purity of the desired enantiomer.

Abstract: A method is provided for preparing carboxylic acid intermediates of the structure ##STR1##

Abstract: A method is provided for preparing homochiral maleimide intermediates of the structure ##STR1## wherein R.sup.7, R.sup.8 and R.sup.9 are as defined herein by reacting a homochiral amine of the structure ##STR2## with maleic anhydride and a silylating agent. The maleimide intermediate is used in the enantio-selective preparation of thromboxane A.sub.2 receptor antagonists.

Abstract: A process for preparing compounds of the formula ##STR1## where a, b, c, R.sub.1, R.sub.2, and R.sub.3 are as defined herein including the step of alkylating a phenol of formula ##STR2## with an acetylene of formula ##STR3## where X is chlorine; bromine; --OC(O)--R.sub.5, where R.sub.5 is alkyl, aryl or substituted aryl; or --OCO.sub.2 R.sub.6, where R.sub.6 is alkyl or ##STR4## in the presence of a catalytic amount of a cuprous or cupric salt. The compounds of formula I are intermediates useful in the preparation of pyranyl cyanoguanidine derivatives.

Abstract: Racemic Feist's acid is treated with (R)-(+) -.alpha.-methylbenzylamine to yield (1R-trans)-3-methylene -cyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzyl-amine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.

Abstract: The protected cyclobutanone of the formula ##STR1## is treated with a dialkylaluminum chloride, an alkylaluminum dichloride, a trialkylaluminum compound, hydrogen in the presence of the catalysts ruthenium black or ruthenium on alumina, diphenyl-silane in the presence of tris(triphenylphosphine) rhodium (I) chloride, or iridium tetrachloride to yield the corresponding diprotected cyclobutanol. This compound is useful as an intermediate in the preparation of antiviral agents.

Abstract: A method is provided for preparing carboxylic acid intermediates of the structure ##STR1##

Abstract: A method is provided for preparing carboxylic acid intermediates of the structure ##STR1##

Abstract: A process for preparing compounds of the formula ##STR1## where a, b, c, R.sub.1, R.sub.2, and R.sub.3 are as defined herein including the step of alkylating a phenol of formula ##STR2## with an acetylene of formula ##STR3## where X is chlorine; bromine; --OC(O)--R.sub.5, where R.sub.5 is alkyl, aryl or substituted aryl; or --OCO.sub.2 R.sub.6, where R.sub.6 is alkyl or ##STR4## in the presence of a catalytic amount of a cuprous or cupric salt. The compounds of formula I are intermediates useful in the preparation of pyranyl cyanoguanidine derivatives.

Abstract: The protected cyclobutanone of the formula ##STR1## is treated with a dialkylaluminum chloride, an alkylaluminum dichloride, a trialkylaluminum compound, diphenylsilane in the presence of tris(triphenylphosphine) rhodium (I) chloride, or iridium tetrachloride to yield the corresponding diprotected cyclobutanol. This compound is useful as an intermediate in the preparation of antiviral agents.

Abstract: A method is provided for preparing carboxylic acid intermediates of the structure ##STR1## wherein an aldehyde of the structure ##STR2## is prepared and subjected to a Horner-Emmons reaction to form the ester of the structure ##STR3## and the ester is hydrogenated to the carboxylic acid which may be used in making the final anti-thrombotic--anti-vasospastic compounds.

Abstract: A method is provided for preparing oxazole intermediates of the structure ##STR1## (wherein R is alkyl) wherein an oxazoline of the structure ##STR2## is oxidized employing an oxidizing agent such as cupric bromide, a base such as 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), and a non-hydride donor amine base such as hexamethylenetetraamine (HMTA). The resulting oxazole may be hydrolyzed to the final anti-thrombotic - anti-vasospastic compounds.

Abstract: A method is provided for preparing bromooxazole intermediates of the structure ##STR1## wherein a vinyl compound of the structure ##STR2## wherein X.sup.1 and X.sup.2 are independently H and Br, is treated with a metal halide such as cupric bromide, and a base such as 1,8-diazabicyclo-[5.4.0]undec-7-ene (DBU). The resulting bromooxazole may be hydrolyzed and hydrogenolyzed to the final anti-thrombotic-anti-vasospastic compounds.