Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]- amino) caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid.

Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid.

Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid.

Abstract: The present invention provides methods for preparing 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine (compound A), which is useful for the treatment of depression and other CNS disorders. The present methods are useful for preparing compound A on large scale in manufacturing facilities.

Abstract: The present invention provides novel methods for preparing N—(S)-1 -azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 1, a nicotinic ?-7 receptor ligand, that are useful for the scaled-up preparation of compound 1. Compound 1 is useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders.

Abstract: The present invention provides novel methods for preparing N—(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 1, a nicotinic ?-7 receptor ligand, that are useful for the scaled-up preparation of compound 1. Compound 1 is useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders.

Abstract: The present invention provides novel methods for preparing indazole-3-carboxylic acid 2, a key starting material for the manufacture of agonists or partial agonists of the nicotinic ?-7 receptor, such as N—(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 13. Nicotinic ?-7 receptor agonists and partial agonists are being useful in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing indazole-3-carboxylic acid on scaled-up levels.

Abstract: The present invention provides novel methods for preparing a key intermediate, 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-?-lactone (2), for the preparation of 1-(2-deoxy-2-fluoro-2-C-methyl-?-D-ribofuranosyl)cytosine (1), which is a potent and selective anti-hepatitis C virus agent.

Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid.

Abstract: A process for preparing polypropylene compositions having high impact strength at low temperatures is disclosed in which the reaction is catalyzed by Ziegler-Natta/metallocene hybrid catalysts by the in-situ polymerization of one or more olefins of the formula CH2?CHR, in which R is hydrogen or an alkyl, cycloalkyl or aryl group having from 1 to 10 carbon atoms, and more specifically comprises preparing an olefin polymer by Ziegler-Natta catalyst components of the titanium or vanadium/metallocene hybrid catalysts while the metallocene components are inactivated beforehand by catalyst inactivators; and polymerizing one or more olefins in the presence of the above olefin polymer, followed by a reactivation of the metallocene components.

Abstract: A method of nitrating a compound selected from the group consisting of is provided.

Abstract: The present invention provides novel methods for preparing compounds (2R)-2-deoxy-2-fluoro-2-methyl-D-erythro-pentono-?-lactone (11) and (2S)-2-deoxy-2-fluoro-2-methyl-D-erythro-pentono-?-lactone (12), which are intermediates for preparing a key intermediate 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-?-lactone (B), for the preparation of 1-(2-deoxy-2-fluoro-2-C-methyl-?-D-ribofuranosyl)cytosine (A), which is a potent and selective anti-hepatitis C virus agent.

Abstract: The present invention provides novel methods for preparing a key intermediate, 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-?-lactone (2), for the preparation of 1-(2-deoxy-2-fluoro-2-C-methyl-?-D-ribofuranosyl)cytosine (1), which is a potent and selective anti-hepatitis C virus agent.

Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid.

Abstract: A method of nitrating a compound selected from the group consisting of is provided.

Abstract: A method of converting pure ?-anomer or ?/?-anomer mixtures of 1,2,3,5-tetra-O-acetyl-L-ribofuranose to methyl-1-(2,3,5-tri-O-acetyl-?-L-ribofuranosyl)-1,2,4-triazole-3-carboxylate an intermediate for levovirin, as well as, the novel pure ?-anomer, alpha 1,2,3,5-tetra-O-acetyl-L-ribofuiranose, are useful in manufacturing levovirin.

Abstract: A method of converting pure &agr;-anomer or &bgr;/&agr;-anomer mixtures of 1,2,3,5-tetra-O-acetyl-L-ribofuranose to methyl-1-(2,3,5 -tri-O-acetyl-&bgr;-L-ribofuranosyl)-1,2,4-triazole-3-carboxylate an intermediate for levovirin, as well as, the novel pure &agr;-anomer, alpha 1,2,3,5-tetra-O-acetyl-L-ribofuiranose, are useful in manufacturing levovirin.

Abstract: Hexahydroindenopyridine compounds having the following formula and relative stereochemistry ##STR1## where R.sup.1 is C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is carboxyl or a group which is metabolized to a carboxyl group under mammalian physiological conditions; R.sup.4 is halogen; mixtures of said compound and acid addition salts thereof exhibit potent antispermatogenic activity and are useful in a method of inhibiting spermatogenesis in mammals.