Patent ID: 7714159
Filing Date: 2010-05-11
Classification: A61P,C07F,C07K,Y02P

Abstract:
1. A large-scale process for preparing a boronic ester compound of formula (I): wherein: R R R R none of the variables R said process comprising: (a) providing a boron “ate” complex of formula (II): where Y is a nucleofugic group; M each of R (b) contacting the boron “ate” complex of formula (II) with a Lewis acid under conditions that afford the boronic ester compound of formula (I) said contacting step being conducted in a reaction mixture comprising: wherein the solubility of water in the ether solvent in (i) or (ii) that has low miscibility with water is less than about 5% w/w; and wherein the ether solvent in (i) or (ii) that has low miscibility with water constitutes at least about 70% v/v of the reaction mixture.