Chiroscience, Ltd.

Chirotech Technology Limited

Janssen Pharmaceutica Nv

Darwin Discovery Limited

Genzyme Corporation

Asta Medica, Aktiengesellschaft

Raymond McCague

Stephen John Taylor

Christopher T Evans

Brian Michael Adger

Ulrich Conrad Dyer

Robin Mark Bannister

Gerard Andrew Potter

Jane Marie Paul

Stanley M Roberts

Martin Woods

Stanley Michael Roberts

Christopher Palmer

Graham Ruecroft

Nicholas David Tyrrell

Horacio F Olivo

Shouming Wang

James Winterman

Nicholas Turner

Derek Thomas Jones

The subject invention pertains to a process for preparing a compound having a formula (4) or (5), in either optically-enriched or racemic form, wherein R,, R,, R,and R,are independently selected from hydrogen, alkyl, aryl, alkaryl, aralkyl and acyl groups. In one embodiment, the process of the invention comprises mixing with a plant extract obtained from crushed daffodil bulbs or crushed snowdrop bulbs an oxidative cyclisation precursor of the compound.

Process for the preparation of galanthamine and its derivatives

Azlactone (3), or the opposite enantiomer thereof, undergoes biotransformation, using suitable enzymatic activity, in the presence of a compound YH to form a N-acyl-amino acid (2), wherein R,, R,and R,are each not hydrogen and are independently selected from groups containing up to 20 carbon atoms, optionally with any combination of R,, R,and R,being joined together to form at least one ring, X is selected from groups containing up to 20 carbon atoms, and Y is selected from the group consisting of &mdash;OH, -Oalkyl and -Nalkyl. Amino acid (1), or the opposite enantiomer thereof, can be prepared in high enantiomeric excess from N-acyl amino acid (2), by converting Y to OH.

Method for preparing tert-leucine and analogues thereof in enantiomeric form and intermediates therein

A process for the preparation of optically-enriched pipecolic acid as a salt with an optically-active acid, comprises asymmetric transformation of pipecolic acid, as a racemic mixture of a mixture enriched in the opposite enantiomer from that desired, with the optically-active acid in a solvent comprising an acid that causes racemisation, in the absence of aldehyde.

Racemization of precursors to levobupivacaine and analogues thereof

Process for the production of lipoic acid

Preparation of chiral cycloalkanols such as endo-5-norbornen-2-ol

Process for preparing galanthamine derivatives by asymmetric reduction

Chiral nitriles, their preparation and their use for the manufacture of

Process for the separation of the enantiomers of a bicyclic lactam

An optically-purified enantiomer of the lactone 4-hydroxy-2-oxabicyclo-�3.3.0!oct-7-en-3-one or an acylate thereof can be obtained by biotransformation. It is a useful synthon in the preparation of an enantiomer of 3-hydroxymethyl-2-hydroxycyclopentene that can be used to prepare carbocyclic nucleosides as a desired enantiomer.

Chiral cyclopentene derivatives and their preparation

A process for the racemization of an enantiomerically-enriched compound of formula (3), comprises treatment of enantiomerically-enriched (3) with a base to obtain anion (4), optionally in protonated form, which is then combined with CH.sub.2 =CH--Y.sup.1 to form racemic (3), ##STR1## wherein Ar=aryl or heteroaryl; Ak=C.sub.1-20 alkyl; X=CN, CO.sub.2 R, CONR.sup.1 R.sup.2, and COR; Y and Y.sup.1 are independently selected from CN, CO.sub.2 R, CONR.sup.1 R.sup.2 and R, R.sub.1 and R.sub.2 are independently selected from H and C.sub.1-20 alkyl; optionally as a salt thereof. This racemization process can be used as part of an efficient synthesis of enantiomerically-enriched verapamil or aminoglutethimide.

Racemisation process

Cycloalkanediols and their use in preparing chiral compounds

Enantiomeric glutarimides such as aminoglutethimide and rogletimide are prepared by cyclisation of a corresponding ester-nitrile which is a good substrate for biotransformation with an enantiospecific esterase.

Chiral compounds and their resolution synthesis using enantioselective

Crystallization process for preparing glycerophosphocholine

Growing community of inventors

Cambridgeshire, United Kingdom

Raymond McCague