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 process for the preparation of compounds of formula ##STR1## or salt thereof where R.sub.1 is --X--Z and X is --C.tbd.C--,R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl;R.sub.3 is hydrogen or alkyl; andZ is a hydrophobic anchor;which includes reacting a compound of formula ##STR2## where R.sub.4 is alkyl, cycloalkyl or aryl; and R.sub.5 is trialkylsilyl or triarylsilyl with a compound of formula ##STR3## where Y is a halogen, to form a compound of formula ##STR4## and hydrolyzing the compound of formula IV to obtain the compounds of formula I. Compounds of formula I or salt thereof where R.sub.1 is --OR.sub.2 ' may be prepared by reacting a compound of formula III with a compound of formulaP(OR.sub.2).sub.3.

Abstract: A process for the preparation of compounds of formula ##STR1## or salt thereof where R.sub.1 is --X--Z and X is --C.tbd.C--,R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl;R.sub.3 is hydrogen or alkyl; andZ is a hydrophobic anchor;which includes reacting a compound of formula ##STR2## where R.sub.4 is alkyl, cycloalkyl or aryl; and R.sub.5 is trialkylsilyl or triarylsilyl with a compound of formula ##STR3## where Y is a halogen, to form a compound of formula ##STR4## and hydrolyzing the compound of formula IV to obtain the compounds of formula I. Compounds of formula I or salt thereof where R.sub.1 is --OR.sub.2 ' may be prepared by reacting a compound of formula III with a compound of formulaP(OR.sub.2).sub.3 XII.

Abstract: A novel, overall process for the preparation of a compound of the formula I: ##STR1## where R.sup.1 and R.sup.2 are each independently hydrogen, an alkyl group, a cycloalkyl group, an aryl group or, taken together with the carbon atom to which they are attached, form a cycloalkyl group; andR.sup.3 is hydrogen, an alkyl group, or an aryl group,or salts thereof, useful as intermediates in the preparation of HMG-CoA reductase inhibitors; novel methods within the overall process; and novel intermediates produced by those methods.

Abstract: A process for the preparation of compounds of formula ##STR1## and pharmaceutically acceptable salts thereof; wherein X is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C-- or --CH.sub.2 O-- (where O is linked to Z); Z is a hydrophobic anchor R.sub.1 is hydrogen, alkyl, cycloalkyl or aryl; comprising the steps of:(A) reacting a compound of formula ##STR2## with a compound of formula ##STR3## or a compound of formula ##STR4## in the presence of an amine base or an alkali metal hydride in an organic solvent to form a compound having the formula ##STR5## (B) heating the compound of formula IX at a temperature of from about 100.degree. C. to about 200.degree. C., to form a compound of formula ##STR6## and (C) quenching the compounds of formula VIII with an acid provides the compounds of formula I.

Abstract: Disclosed herein is a process for preparing a novel monoester of the formula ##STR1## in which the associated novel diester ##STR2## is hydrolyzed in the presence of one or more water-soluble enzymes or microorganisms capable of selectively hydrolyzing the --O--C(O)--R.sup.1 group, wherein the treatment is carried out in a biphasic solvent system comprising an aqueous phase having the enzymes or microorganisms and an organic phase immiscible in water having the diester. Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z),3.alpha.,4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]amino]me thyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using this enzymatic/microbial process.

Abstract: Disclosed herein is a process for preparing a novel monoester of the formula ##STR1## in which the associated novel diester ##STR2## is hydrolyzed in the presence of one or more water-soluble enzymes or microorganisms capable of selectively hydrolyzing the --O--C(O)--R.sup.1 group, wherein the treatment is carried out in a biphasic solvent system comprising an aqueous phase having the enzymes or microorganisms and an organic phase immiscible in water having the diester. Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z),3.alpha.,4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]-amino]m ethyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using this enzymatic/microbial process.

Abstract: Disclosed herein is a novel process in which novel aldehydes ##STR1## and the trans isomer thereof are hydrolyzed by treatment with an alkali metal carbonate, bicarbonate or hydroxide and water to form the cis enantiomer ##STR2## Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z), 3.alpha., 4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]-amino ]methyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using the above process.

Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.

Abstract: In accordance with the present invention an improved process for preparing resolved compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or acetyl.

Abstract: A process is provided for preparing a 7-oxabicycloheptane amino alcohol intermediate of the general structure ##STR1## (wherein the above structures represents (D) or (L) isomers)which is useful in preparing thromboxane A.sub.2 receptor antagonists. This intermediate is prepared by reacting mesanhydride with an aryl amine ##STR2## wherein R is alkyl, CH.sub.2 OH, CO.sub.2 H or CO.sub.2 alkyl, to form the acid ##STR3## which is reduced by treatment with lithium aluminum hydride or diisobutylaluminum hydride or Red-Al to form the alcohol ##STR4## wherein R.sup.1 is CH.sub.2 OH when R is CO.sub.2 H, CO.sub.2 alkyl or CH.sub.2 OH, and R.sup.1 is alkyl when R is alkyl; where in the above alcohol R.sup.1 is CH.sub.2 OH, such alcohol compound is treated with an alkyl chloroformate in the presence of base such as an alkali metal alkoxide to form the alcohol ##STR5## which undergoes cleavage by treatment with alkali metal, ammonia and acid to form the amino alcohol intermediate.Where in the above alcohol R.sup.

Abstract: A process is provided for preparing phosphonyloxyacylamino acids and derivatives thereof having the structure ##STR1## wherein X is ##STR2## which includes the steps of treating a phosphonic acid dichloride of the structure ##STR3## with an .alpha.-hydroxy acid of the structure ##STR4## in the presence of base such as triethylamine at reduced temperatures to form the cyclic mixed anhydride of the structure ##STR5## (which is a new intermediate) and reacting the cyclic mixed anhydride with an amino acid or ester of the structureHXin the presence of base such as triethylamine produces the ACE inhibitor compound ##STR6## In an alternative process, the cyclic anhydride is quenched with water to form the diacid ##STR7## which is treated with a condensing agent such as dicyclohexyl carbodiimide (DCC), 1,1-carbonyldiimidazole (CDI) or thionyl chloride followed by quenching with the amino acidHXproduces the above ACE inhibitor compound.

Abstract: In accordance with the present invention an improved process for preparing resolved compounds of the formula ##STR1## being the cis(+) isomer, is disclosed, wherein R.sub.1 and R.sub.2 are each independently hydrogen, halogen, alkyl, alkoxy, aryloxy, arylalkoxy, diarylalkoxy, arylalkyl, cyano, hydroxy, alkanoyloxy, ##STR2## fluoro substituted alkoxy, fluoro substituted alkyl, (cycloalkyl)alkoxy --NO.sub.2, NX.sub.3 X.sub.4, --S(O).sub.m alkyl, ##STR3## m is 0, 1 or 2; X.sub.1 and X.sub.2 are each independently hydrogen, alkyl, aryl or heteroaryl, or X.sub.1 and X.sub.2 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl;X.sub.3 and X.sub.4 are each independently hydrogen, alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl, or ##STR4## X.sub.5 is hydroxy, alkoxy, aryloxy, amino, alkylamino or dialkylamino; andX.sub.6 is alkyl, alkoxy or aryloxy; with the proviso that if R.sub.4 is a 7-alkyl group, it must have a tertiary carbon atom bonded to the ring.

Abstract: A process is provided for preparing phosphonyloxyacylamino acids and derivatives thereof having the structure ##STR1## wherein ##STR2## which includes the steps of treating a phosphonic acid dichloride of the structure ##STR3## with an .alpha.-hydroxy acid of the structure ##STR4## in the presence of base such as triethylamine at reduced temperatures to form the cyclic mixed anhydride of the structure ##STR5## (which is a new intermediate) and reacting the cyclic mixed anhydride with an amino acid or ester of the structureHXin the presence of base such as triethylamine produces the ACE inhibitor compound ##STR6##In an alternative process, the cyclic anhydride is quenched with water to form the diacid ##STR7## which is treated with a condensing agent such as dicyclohexyl carbodiimide (DCC), 1,1-carbonyldiimidazole (CDI) or thionyl chloride followed by quenching with the amion acidHXproduces the above ACE inhibitor compound.

Abstract: A method is provided for preparing phosphinic acid compounds, which are useful in preparing certain angiotensin converting enzyme inhibitors, which have the formula ##STR1## wherein R.sub.1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;X is hydrogen, lower alkyl or phenyl;Y is hydrogen, lower alkyl, phenyl or alkoxy, or together X and Y are --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.dbd.CH--, or ##STR2## and n is 0 or 1including salts thereof and stereoisomers thereof, which method includes the steps of reacting a phosphinic acid ester of the structure ##STR3## wherein R.sub.

Abstract: A process is provided for preparing a 7-oxabicycloheptane amino alcohol intermediate of the general structure ##STR1## which is useful in preparing thromboxane A.sub.2 receptor antagonists. This intermediate is prepared by reacting mesoanhydride with an aryl amine ##STR2## wherein R is alkyl, CH.sub.2 OH, CO.sub.2 H or CO.sub.2 alkyl, to form the acid ##STR3## which is reduced by treatment with lithium aluminum hydride or diisobutylaluminum hydride or Red-Al to form the alcohol ##STR4## wherein R.sup.1 is CH.sub.2 OH when R is CO.sub.2 H, CO.sub.2 alkyl or CH.sub.2 OH, and R.sup.1 is alkyl when R is alkyl; where in the above alcohol R.sup.1 is CH.sub.2 OH, such alcohol compound is treated with an alkyl chloroformate in the presence of base such as an alkali metal alkoxide to form the alcohol ##STR5## which undergoes cleavage by treatment with alkali metal, ammonia and acid to form the amino alcohol intermediate.Where in the above alcohol R.sup.

Abstract: A compound (for preparing an ACE inhibitor), namely, triphenyl cerium and a process for preparing same by reacting cerium trichloride (CeCl.sub.3) with phenyllithium, are provided.

Abstract: A process is provided for preparing a 7-oxabicycloheptane amino alcohol intermediate of the general structure ##STR1## (wherein the above structure represents (D) of (L) isomers) which is useful in preparing thromboxane A.sub.2 receptor antagonists. This intermediate is prepared by reacting mesoanhydride with an aryl amine ##STR2## wherein R is alkyl, CH.sub.2 OH, CO.sub.2 H or CO.sub.2 alkyl, to form the acid ##STR3## which is reduced by treatment with lithium aluminum hydride or diisobutylaluminum hydride or Red-Al to form the alcohol ##STR4## wherein R.sup.1 is CH.sub.2 OH when R is CO.sub.2 H, CO.sub.2 alkyl or CH.sub.2 OH, and R.sup.1 is alkyl; where in the above alcohol R.sup.1 is CH.sub.2 OH, such alcohol compound is treated with an alkyl chloroformate in the presence of base such as an alkali metal alkoxide to form the alcohol ##STR5## which undergoes cleavage by treatment with alkali metal, ammonia and acid to form the amino alcohol intermediate.Where in the above alcohol R.sup.

Abstract: A process is provided for preparing a 7-oxabicycloheptane amino alcohol intermediate of the general structure ##STR1## which is useful in preparing thromboxane A.sub.2 receptor antagonists. This intermediate is prepared by reacting mesonhydride with an aryl amine ##STR2## wherein R is alkyl, CH.sub.2 OH, CO.sub.2 H or CO.sub.2 alkyl, to form the acid ##STR3## which is reduced by treatment with lithium aluminum hydride or diisobutylaluminum hydride or Red-Al to form the alcohol ##STR4## wherein R.sup.1 is CH.sub.2 OH when R is CO.sub.2 H, CO.sub.2 alkyl or CH.sub.2 OH, and R.sup.1 is alkyl when R is alkyl; where in the above alcohol R.sup.1 is CH.sub.2 OH, such alcohol compound is treated with an alkyl chloroformate in the presence of base such as an alkali metal alkoxide to form the alcohol ##STR5## which undergoes cleavage by treatment with alkali metal, ammonia and acid to form the amino alcohol intermediate.Where in the above alcohol R.sup.

Abstract: A process is provided for preparing phosphonous acids of the structure wherein R.sub.1 is lower alkyl or arylalkyl ##STR1## which are useful in preparing phosphinic and phosphonic acid ACE inhibitors, which process includes the steps of treating an olefin of the structure R.sub.1 --CH.dbd.CH.sub.2 wherein R.sub.2 is lower alkyl or arylalkyl with a phosphorus-containing reagent such as sodium hypophosphite or hypophosphorous acid in the presence of an organic alcohol solvent such as ethanol or methanol, and a radical initiator such as azobisisobutyronitrile, under acidic conditions, preferably at the reflux temperature of the organic solvent, to form the phosphonous acid without forming the alkyl ester.