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US 6,187,936 B1Granted
Process for the enzymatic kinetic resolution of 3-phenylglycidates by transesterification with aminoalcohols
AssigneeZambon Group S.p.A.
InventorsMarco Villa, Dario Tentorio, Angelo Restelli, Sergio Riva
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Abstract
A process for the preparation of I: in which R and R1 have the meanings reported in the description, that comprises the enzymatic kinetic resolution by transesterification with aminoalcohols of 3-phenylglycidates of formula I: is described.
Claims17
A process for the preparation of:
- which comprises the enzymatic kinetic resolution of trans 3-phenylglycidates of formula:
- wherein
- R is linear or branched C1-C4alkyl;
- R1 is hydrogen, linear or branched C1-C3 alkyl, linear or branched C1-C3 alkoxy, aryl or halogen;
- by transesterification of the mixture of trans enantiomers of formula I catalysed by enzymes in organic solvent with aminoalcohols of formula:
- wherein
- n is an integer from 2 to 4;
- R2 is hydrogen or linear or branched C1-C4 alkyl;
- R3 is linear or branched C1-C4 alkyl;
- or
- R2 and R3 together with the nitrogen atom form a 5 to 7 membered saturated cycle;
- to give a mixture of trans esters, non transesterified and transesterified, having an opposite absolute configuration, of formula III and IV respectively:
- wherein R, R1, R2, R3 and n have the above reported meanings,
- and the subsequent separation of such a mixture of esters of formula III and IV.
11 more elements
Dependencies are inferred from the claim text.