Hoffmann-la Roche Inc.

Roche Colorado Corporation

Roche Palo Alto LLC

Genentech, Inc.

F. Hoffmann-la Roche Ag

Kurt Puentener

Michelangelo Scalone

Lewis M Hodges

Yeun-Kwei Han

Michael P Fleming

David A Johnston

Robert J Topping

Mark A Schwindt

Roger P Micheli

Chris R Roberts

Serena Maria Fantasia

Simon Breitler

Hasane Ratni

Alexander Flohr

Ralf Karch

Konrad H Bleicher

Angelino Doppiu

Eileen Woerner

Andreas Rivas-Nass

Hans Iding

Beat Wirz

Bjoern Bartels

Stephan Bachmann

Peter John Harrington

Stefan Hildbrand

Pius Waldmeier

Bruno Lohri

Fabienne Hoffmann-Emery

Ursula Hoffmann

Shaoning Wang

Roland Winde

Alec Fettes

René Trussardi

Ernst Kupfer

Allen Yu Hong

Joerg Lill

Kazimierz Michal Pietrusiewicz

Paolo Tosatti

Wioleta Swierczynska

Christian Oliver Kappe

Rene Lebl

Jason Douglas Williams

Anton Cueni

Anna-Lena Glass

Rene (deceased) Trussardi

The invention comprises a process for the preparation of a GalNAc phosphoramidite epimer of the formula (I), wherein Ris a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20, corresponding enantiomers and/or optical isomers thereof and the use of the process for the preparation of GalNAc-cluster oligonucleotide conjugates.

Process for the preparation of GalNAc phosphoramidite epimers

The invention comprises a process for the preparation of therapeutically valuable GalNAc cluster oligonucleotide conjugates. The process comprises the coupling of an alkali metal salt, earth alkali metal salt or a tetraalkylammonium salt of an oligonucleotide with a GalNAc cluster compound or with a salt thereof and a subsequent purification.

Process for GalNAc oligonucleotide conjugates

The invention relates to compounds of the formula 

Process for making lysine-glutamic acid dipeptide derivatives

The invention relates to compounds of the formula I. The compounds of formula I are versatile peptide intermediates for the solid phase peptide synthesis (SPPS) of peptide drugs which comprise a Glu-fatty alkyl side chain building block attached to a Lys-part of the peptide chain. 

Lysine-glutamic acid dipeptide derivatives

A novel process for the preparation of imidazo[1,2-a]pyridine compounds of the formula  The imidazo[1,2-a]pyridine compounds of the formula I are either precursors for active principles or active principles itself, acting as phosphodiesterase (PDE) inhibitors, particularly PDE10 inhibitors which have the potential to treat psychotic disorders like schizophrenia (Int. Patent Publication WO 2012/076430).

Pd-catalyzed coupling of pyrazole amides

The invention relates to a novel process for the preparation of 2-phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I or of a salt thereof  2-Phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I with their 1,2,4-triazole nucleus build the structural core of a great number of functionalized molecules in medicinal chemistry.

Process for the preparation of 2-phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives

The invention relates to a process for the preparation of a compound of formula (I) or a salt thereof.

Process for the preparation of propionic acid derivatives

The invention relates to a novel process for the preparation of (3S,4S)- or (3R,4R)-1-benzyl-4-(halogen-aryl)-pyrrolidine-3-carboxylic acids of formula I or salts thereof, wherein X and Y are each independently hydrogen or a halogen atom, with the proviso that at least one of X or Y is a halogen atom. The compounds of formula I are useful as starting materials or intermediates for the preparation of pharmaceutically active compounds, especially for compounds, which are useful for the treatment of central nervous system disorders.

Process for the preparation of pyrollidine-3-carboxylic acids

The invention relates to a novel process for the preparation of Ruthenium metathesis catalysts of the formula  Ruthenium metathesis catalysts have been widely applied in the synthesis of macrocyclic drug compounds.

Process for the preparation a ruthenium complex

The invention relates to novel metathesis catalysts of the formula a process for making the same and their use in metathesis reactions such as ring closing or cross metathesis. The invention further relates to a process for the manufacture of a macrocyclic compound of formula VII which have the potential to be useful as HCV protease inhibitors.

Ruthenium complexes as catalysts for metathesis reactions

The present invention relates to a new process for the preparation of macrocyclic HCV protease inhibitor compounds of the formula wherein Ris an amino protecting group and X is halogen by way of a ring closing metathesis approach.

Process for the preparation of a macrocycle

Disclosed are novel metathesis catalysts of the formula wherein R, R, R, R, R, R, X, X, L and Y are as described herein, a process for making the same and their use in metathesis reactions such as ring closing or cross metathesis.

Metathesis catalysts

The invention is concerned with new phosphine ligands of the formula I wherein

Phosphine ligands

The invention relates to the preparation of enantiomerically pure (S)-1,1,1-trifluoro-2-propanol by asymmetric hydrogenation of 1,1,1-trifluoroacetone which process comprises hydrogenating 1,1,1-trifluoroacetone in the presence of a ruthenium phosphine complex catalyst represented by formulaRu(E)(E')(L)(A)

Asymmetric hydrogenation of 1,1,1-trifluoroacetone

The present invention is concerned with a novel process for the preparation of compounds of formula I comprising catalytic asymmetric hydrogenation of a compound of formula (II) in the presence of a catalyst comprising ruthenium and a chiral diphosphine ligand or comprising rhodium and a chiral diphosphine ligand, wherein R, R, Rand Rare as defined in the specification and claims. The compounds of formula I and the corresponding salts and/or esters are pharmaceutically active substances.

Process for the production of chiral propionic acid derivatives

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Basel, Switzerland

Kurt Puentener