Hoffmann-la Roche Inc.

Genentech, Inc.

F. Hoffmann-la Roche Ag

Pankaj Rege

Stefan Hildbrand

Francis Gosselin

Haiming Zhang

Keshab Sarma

Stephan Bachmann

Scott J Savage

Chong Han

Fabienne Hoffmann-Emery

Ngiap-Kie Lim

Ursula Hoffmann

Roland Meier

Serena Maria Fantasia

Andrew McClory

Lianhe Shu

Pascal Dott

Daniel Vincent Fishlock

Gerard Moine

Georg Wuitschik

Christian Moessner

Theresa Humphries

Christian Jenny

Chen Gu

Fabian Feyen

The present invention relates to a process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.

Process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one compounds

Processes are described for the preparation of estrogen receptor modulating compound, (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid I: 

Process for the preparation of (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid

The invention relates to a process for the preparation of 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid of the formula (I) as well as intermediates thereof and pharmaceutical preparations thereof, comprising the step of reacting a compound of the formula (IV) with a compound of the formula (V), as defined in the specification, in the presence of a chiral silver- or copper catalyst.

Asymmetric synthesis of a substituted pyrrolidine-2-carboxamide

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Basel, Switzerland

Pankaj Rege