Process for the preparation of aniline boronic acids and derivatives thereof

摘要

Production of anilineboronic acid derivatives (I) comprises converting an aniline compound (II) to a doubly protected derivative (III), metallating (III) and simultaneously or subsequently reacting it with a borate ester (IV) to give a protected anilineboronic acid ester (V), and deprotecting (V). Production of anilineboronic acid derivatives of formula (I) comprises converting an aniline compound of formula (II) to a doubly protected derivative of formula (III), metallating (III) and simultaneously or subsequently reacting it with a borate ester of formula (IV) to give a protected anilineboronic acid ester of formula (V), and deprotecting (V): [Image] PG : protecting group; R : H, halo, 1-20C alkyl or alkoxy, optionally substituted 6-12C aryl or aryloxy, heteroaryl or heteroaryloxy, optionally substituted 3-8C cycloalkyl, dialkylamino, diarylamino, alkylthio, arylthio, ester or acetal; X : H or halo; R1>-R3>H or optionally substituted 1-20C alkyl, or two of R1>-R3> can form a ring or another borate group.