Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.

Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.

Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, namely, (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide. Also, disclosed are polymorphs of this compound and methods for isolating a specific polymorph. Also, disclosed are pharmaceutical compositions and methods for preparing pharmaceutical compositions.

Abstract: Provided are polymorphs of an A1 adenosine receptor partial agonist, compositions thereof, methods for their preparation, and methods for their uses.

Abstract: The present invention is directed to a process for preparing (S,S)-cis-2-phenyl-3-aminopiperidine and (S,S)-cis-2-phenyl-3-tertbutoxycarbonylaminopiperidine.

Abstract: A process for preparing (S,S)-cis-2-benzhydryl-3-benzylaminoquinuclidine. The process includes the steps of contacting a compound containing a mixture of R- and S-isomers and having the formula with an effective amount of a chiral organic acid in the presence of an organic solvent and an effective amount of an organic carboxylic acid for converting the R-isomer into an acid salt of the S isomer, wherein the organic solvent is capable of solubilizing the compound containing the mixture of R- and S-isomers, while precipitating the acid salt and the organic carboxylic acid is different from the chiral organic acid; neutralizing the acid salt with a base to provide an S-isomer-of a chiral ketone of the formula reacting the chiral ketone with an organic amine in the presence of a Lewis acid to provide the corresponding imine and reducing the imine.

Abstract: A process for preparing (S,S)-cis-2-benzhydryl-3-benzylaminoquinuclidine. The process includes the steps of contacting a compound containing a mixture of R- and S-isomers and having the formula with an effective amount of a chiral organic acid in the presence of an organic solvent and an effective amount of an organic carboxylic acid for converting the R-isomer into an acid salt of the S isomer, wherein the organic solvent is capable of solubilizing the compound containing the mixture of R- and S-isomers, while precipitating the acid salt and the organic carboxylic acid is different from the chiral organic acid; neutralizing the acid salt with a base to provide an S-isomer of a chiral ketone of the formula ; and reacting the chiral ketone with an organic amine in the presence of a Lewis acid to provide the corresponding imine and reducing the imine.

Abstract: A process for preparing (S,S)-cis-2-benzhydryl-3-benzylaminoquinuclidine.

Abstract: The present invention is directed to a process for preparing (S,S)-cis-2-phenyl-3-aminopiperidine and (S,S)-cis-2-phenyl-3-tertbutoxycarbonylaminopiperidine.

Abstract: Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.

Abstract: Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.

Abstract: Ortho esters and ortho carbonates can be produced by alkylating esters and carbonates with, for example, the hexafluorophosphate salt of a trialkyl oxonium ion. The spiro species are useful intermediates in the synthesis of complex organic molecules. Synthetic pathways for the production of medically active compounds incorporates spiro ortho esters. Anti-first-pass effect materials are produced in high yield utilizing a synthetic strategy incorporating cyclic ortho ester intermediates.

Abstract: The present invention provides a method for enantioselectively producing a nonracemic 6,7-dihydroxy geranyloxy compound from a geranyloxy compound. In particular, methods of the present invention involve enantioselectively epoxidizing the geranyloxy compound and hydrolyzing the epoxide moiety under conditions sufficient to produce the nonracemic 6,7-dihydroxy geranyloxy compound.

Abstract: The present invention provides a method for enantioselectively producing a nonracemic 6,7-dihydroxy geranyloxy compound from a geranyloxy compound. In particular, methods of the present invention involve enantioselectively epoxidizing the geranyloxy compound and hydrolyzing the epoxide moiety under conditions sufficient to produce the nonracemic 6,7-dihydroxy geranyloxy compound.

Abstract: This invention provides a process for preparing acylaromatics comprising reacting an aromatic compound with a carboxylic acid in the presence of a reaction medium comprising polyphosphoric acid and a strong protic acid. In one embodiment, the invention provides a process for preparing a para-acyl phenoxyethylamine comprising the steps of reacting a 2-phenoxyethyl compound bearing a leaving group on the ethyl 1-position with a carboxylic acid in the presence of a reaction medium comprising polyphosphoric acid and a strong protic acid, to form apara-acyl phenoxyethyl intermediate bearing the leaving group; and reacting the para-acyl phenoxyethyl intermediate with an amine that substitutes for the leaving group to form the para-acyl phenoxyethylamine.

Abstract: Process for the enzymatic production of isomerically pure compounds having the general formulae I and II ##STR1## in which the substituents R have the meanings stated in the claims, as well as their use for the production of isomerically pure isosorbide-2-nitrate having the formula V and isosorbide-5-nitrate having the formula VI, ##STR2## which are both important as therapeutic agents for coronary diseases.

Abstract: Process for the enzymatic production of isomerically pure compounds having the general formulae I and II ##STR1## in which the substituents R have the meanings stated in the claims, as well as their use for the production of isomerically pure isosorbide-2-nitrate having the formula V and isosorbide-5-nitrate having the formula VI, ##STR2## which are both important as therapeutic agents for coronary diseases.

Abstract: Provided are enzymatic methods for the selective hydrolytic resolution of certain enantiomers of a pharmaceutical compound, the pharmaceutical compound comprising a (.+-.) mixture of a .alpha.-substituted 2-methyl proprionic acid derivative. Specifically provided is the selective enzymatic resolution of either the R(+) or S(-) enantiomer of (.+-.)-ethyl ciprofibrate. Also provided are substantially pure enantiomers of R(+) and S(-) ciprofibrate.

Abstract: There is provided a regio-selective method for the resolution of carbohydrate monoester mixtures, by treating such mixtures with one or more selective enzymes. The resolution of such mixtures results in monoesters comprising significantly purer isolates of one desired isomer.

Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.