Chirotech Technology Limited

Teva Pharmaceutical Industries Limited

Dr. Reddy's Laboratories, Incorporated

Ian Campbell Lennon

Philip Mark Jackson

Eliezer Bahar

Lee Terence Boulton

Ulrich Berens

Martin E Fox

Stephen Benedict David Winter

The invention concerns an enantiomerically enriched compound of formula (1) or the opposite enantiomer thereof wherein each of Ar&#x2014;Arrepresent the same or different aromatic groups of up to 20 carbon atoms and the bridging group X is the formula (5) in which * denotes points of attachment to phosphorus atoms and methods of making thereof.

Bisphospholanes for use as catalysts in asymmetric reactions

A process for manufacturing (R)-propynylaminoindans, and alternatively, a process for manufacturing (S)-propynylaminoindans. The chiral propynylaminoindans include alkoxy or alkylcarbamates derivatives. The process comprises transfer or pressure hydrogenation in the presenc of an optically active catalyst to reduce 1-indanones. The chiral product, either (S)- or (R)-indanols undergo nucleophilic substitution to produce the named product. In an additional aspect, the invention relates to novel intermediates and compounds, namely, substituted indanones, substituted (S)-indanols and substituted (R)-indanols.

Process for the synthesis of enantiomeric indanylamine derivatives

A process for manufacturing (R)-propynylaminoindans, and alternatively, a process for manufacturing (S)-propynylaminoindans. The chiral propynylaminoindans include alkoxy or alkylcarbamates derivatives. The process comprises transfer or pressure hydrogenation in the presence of an optically active catalyst to reduce 1-indanones. The chiral product, either (S)- or (R)-indanols undergo nucleophilic substitution to produce the named product. In an additional aspect, the invention relates to novel intermediates and compounds, namely, substituted indanones, substituted (S)-indanols and substituted (R)-indanols.

Preparation of phosphine ligands

Intermediate for the synthesis of prostaglandins

The present invention pertains to a process for the preparation of an arylphosphine of the formula R,OC&mdash;Ar&mdash;PR,R,wherein Ar is aryl or heteroaryl; R,is an alkoxy or amine group; and R,and R,are each any organic group; and each of the respective groups may optionally be substituted with any non-interfering group; which comprises the reaction of a sulfonyloxy compound of the formula R,OC&mdash;Ar&mdash;OSO,R,wherein R,is alkyl, haloalkyl, perhaloalkyl, aryl, aralkyl or alkaryl, with a phosphine of the formula HPR,R,, in a solvent and in the presence of a palladium catalyst and a base. The arylphosphine can then readily be converted to a chiral phosphine ligand.

Preparation of arylphosphines

An enantiomerically enriched compound of formula 1,

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Cambridge, United Kingdom

Ian Campbell Lennon