Process for the preparation of 2-cyanophenylboronic acid and esters thereof

摘要

The present invention relates to a process for the synthesis of 2-cyanophenylboronic acid and the esters and salts thereof of formula (II), which are intermediates of the synthesis of active pharmaceutical ingredients such as Perampanel or E2040. formula (II): (II).;

主权项

1. Process for the preparation of an ester of 2-cyanophenylboronic acid of formula (II):wherein R1 and R2 are independently linear or branched C1-C6 alkyl groups or are joined to form a cycle containing between 1 and 6 possibly substituted carbon atoms, comprising:
(a) converting a 2-halogenbenzonitrile of formula (IV):  wherein X is selected from the group consisting of chlorine, bromide and iodine, in a 2-cyanophenyl magnesium halide lithium chloride complex of formula (III): wherein X′ is selected from the group consisting of chlorine, bromine and iodine; and (b) converting the compound obtained in step (a) to give the compound of formula (II).