Hoffmann-La Roche Inc.

Isotechnika Inc.

F. Hoffmann-La Roche Ag

Bruno Lohri

Rudolf Schmid

Wolfgang Wostl

Stefan Hildbrand

Jean-Michel Adam

Hans-Jurgen Mair

Patrizio Mattei

Eric Vieira

Michelangelo Scalone

Robert T Foster

Randall W Yatscoff

Beat Wirz

Hans Iding

Selvaraj A Naicker

Kurt Puentener

Ulrich Zutter

Ursula Hoffmann

Joseph Foricher

Alec Fettes

Peter Vogt

Stefan Abrecht

Ernst Kupfer

Mark D Abel

Rolf G&uuml;ller

Gerard Moine

Markus Schlageter

Kazimierz Michal Pietrusiewicz

Hans-Jürgen Mair

Wioleta Swierczynska

Seetharaman Jayaraman

Christian-Johannes Jenny

The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R, R, R, R, Rand n are as defined in the description and claims and to intermediates useful in the method of the invention as well as salts thereof.

Method for preparing enantiomerically pure 4-pyrrolidino phenylbenzyl ether derivatives

The present invention relates to a process for the preparation of 1-(2-ethyl-butyl)-cyclohexanecarboxylic acid which is useful as an intermediate in the preparation of pharmaceutically active compounds.

Process

The present invention relates to a process for the preparation of 1-(2-ethyl-butyl)-cyclohexanecarboxylic acid which is useful as an intermediate in the preparation of pharmaceutical active compounds.

Process for the preparation of CETP(1)

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

Phosphine ligands

This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

Process for the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one useful in the preparation of the DPP-IV inhibitor (S)-1 ((2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7, 11b-hexahydro-2H-pyrido[2,1-a] isoquinolin-3-yl)-4-fluoromethyl-pyrrolidin-2-one

The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R, R, R, R, Rand n are as defined the description and claims and to intermediates and salts thereof useful in the method of the invention.

Method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives

The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISA247, and derivatives thereof. ISA247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. Stereoselective pathways may utilize a Wittig reaction, or an organometallic reagent comprising inorganic elements such as boron, silicon, titanium, and lithium. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.

Synthesis of cyclosporin analogs

The present invention concerns intermediates useful in and a process for the preparation of a compound of formula 1 or a salt thereof

Process and intermediates for preparation of substituted piperidines

Process and intermediates for preparation of substituted piperidine-epoxides

A process for oxidizing primary and secondary alcohols to the corresponding aldehydes and ketones is disclosed. The oxidation is carried out by reacting the primary or secondary alcohol with an organic N-chloro compound oxidizing agent in the presence of a catalyst of the formula: ##STR1## wherein the substituent groups are as defined in the specification.

Process for the oxidation of alcohols

The present invention is concerned with a novel process for the making of a compound of formula I ##STR1## by oxidizing the corresponding 3-hydroxymethyl-cephem derivative with an inorganic hypohalite or inorganic halite in the presence of compounds of formula III ##STR2## is wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and Y are as defined herein. The process is useful for providing 3-formyl-cephem compounds useful in the making of cephalosporin derivatives.

Process for making 3-formylcephem derivatives

A process for synthesizing 3,5,5-trimethyl-4-[(E)-3-oxo-1-butenyl]-2-cyclohexen-1-one which is a known intermediate in a process for preparing a carotenoid.

Carotenoid intermediate by an oxidation process

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Reinach, Switzerland

Bruno Lohri