Hoffmann-la Roche Inc.

Emisphere Technologies, Inc.

F. Hoffmann-la Roche Ag

Pingsheng Zhang

Miall Cedilote

Zhiming Dong

Yi Ren

Thomas Cleary

Joseph Norman Bernadino

Jodie Brice

George Frederick Klein

Juergen Wichmann

Thomas Johannes Woltering

Hans Iding

William Elliot Bay

Paul Spurr

Stephan Bachmann

Stefan Hildbrand

William Elliott Bay

Jason Yang

Amit Srivastava

Doreen Miller

Daniel Bailey

Thomas P Cleary

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.

Process for the manufacture of SNAC (salcaprozate sodium)

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. 

Methods for the preparation of 5-[2-[7 (trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo [1,5-A]pyrimidin-3-yl[ethynyl]-2-pyridinamine

The present invention provides novel methods for preparing N&#x2014;(S)-1 -azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide HCl salt 1, a nicotinic &#x3b1;-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.

Methods for the preparation of N-(S)-1-azabicyclo[2.2.2]oct-3-yl-1H-indazole-3-carboxamide hydrochloride salt

The present invention provides novel methods for preparing a key intermediate, 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-&#x3b3;-lactone (2), for the preparation of 1-(2-deoxy-2-fluoro-2-C-methyl-&#x3b2;-D-ribofuranosyl)cytosine (1), which is a potent and selective anti-hepatitis C virus agent.

Process for the preparation of 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-gamma-lactone

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.

Methods for producing N-(8-[2-hydroxybenzoyl]-amino) caprylic acid

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

Mono-nitration of aromatic compounds via nitrate salts

A method of converting pure &#x3b1;-anomer or &#x3b2;/&#x3b1;-anomer mixtures of 1,2,3,5-tetra-O-acetyl-L-ribofuranose to methyl-1-(2,3,5-tri-O-acetyl-&#x3b2;-L-ribofuranosyl)-1,2,4-triazole-3-carboxylate an intermediate for levovirin, as well as, the novel pure &#x3b1;-anomer, alpha 1,2,3,5-tetra-O-acetyl-L-ribofuiranose, are useful in manufacturing levovirin.

Process for producing a ribofuranose

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Florence, SC, United States of America

Pingsheng Zhang