Dsm IP Assets B.v.

Astra Zeneca U.k. Limited

Peter Johannes Dominicus Maas

Ben De Lange

Andreas Hendrikus Maria De Vries

Daniel Mink

Johannes Gerardus De Vries

Jacob Hermanus Mattheus Hero Kooistra

David Hyett

Friso Bernard Jan Van Assema

Dominique Monique Charles Callant

Hermanus Carolus Catherina Karel Bakel Van

David John Hyett

The present invention relates to a process for the preparation of an enantiomerically enriched optionally substituted indoline-2-carboxylic acid or a salt thereof, wherein an enantiomerically enriched chiral ortho-X-substituted phenylalanine compound, wherein X is a leaving group, is subjected to cyclisation, preferably at a temperature of below about 140&#xb0; C., upon formation of the enantiomerically enriched indoline-2-carboxylic acid compound.

Process for the preparation of enantiomerically enriched indoline-2-carboxylic acid

Process for the preparation of an ester of formula (1), wherein Rrepresents a leaving group, CN, OH or a COORgroup, Rand Reach independently represent a 1-3 C alkyl group, and Rand Reach independently represent an ester residue, wherein the corresponding salt with formula (2), wherein M represents H or an alkali (earth) metal in an inert solvent is contacted with an acid chloride forming agent to form the corresponding acid chloride, and the acid chloride is contacted with an alcohol with formula ROH in the presence of N-methyl-morpholine. Preferably M represents an alkali metal, and Rrepresents an alkyl group, particularly a t.-butyl group. (1), (2) 

Process for the preparation of dioxane acetic acid esters

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Puth, Netherlands

Peter Johannes Dominicus Maas