PROCESS FOR PREPARING FLUOROLEUCINE ALKYL ESTERS

摘要

This invention relates to a resolution process for the preparation of fluoroleucine alkyl esters.

主权项

1. A process for preparing a compound of formula I: comprising the steps of: a. alkylating an imine carboxylate of formula II with an alkylallyl halide to form a substituted imine of formula III; b. deprotecting the substituted imine of formula III with an acid to yield an amine of formula IV; c. resolving the amine of formula IV with a chrial protic acid; d. fluorinating the resolved amine to yield the compound of formula I.wherein R1 is C1-5 alkyl;R2 is C1-5 fluoroalkyl;R3 is aryl or heteroaryl;R4 is aryl or heteroaryl;R5 is C1-3 alkyl;X is H2SO4, L-tartaric acid, D-BOC proline, L-(−)-10-camphorsulfonic acid or N-acetyl-D-phenyl alanine