Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Zhiming Dong

Pingsheng Zhang

Miall Cedilote

Jodie Brice

Juergen Wichmann

Thomas Johannes Woltering

Paul Spurr

Stephan Bachmann

Stefan Hildbrand

Jason Yang

Amit Srivastava

Doreen Miller

Daniel Bailey

Pingsheng Zhan

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

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

Zhiming Dong