Patent ID: 8283467
Filing Date: 2012-10-09
Classification: A61P,C07F,C07K,Y02P

Abstract:
1. A large-scale process for forming a compound of formula (XIV): or a boronic acid anhydride thereof, said process comprising: wherein: said contacting step being conducted in a reaction mixture comprising an ether solvent that has low miscibility with water, wherein the solubility of water in the ether solvent that has low miscibility with water is less than about 5% w/w, and wherein the ether solvent that has low miscibility with water constitutes at least about 70% v/v of the reaction mixture; or an acid addition salt thereof; wherein: to form a compound of formula (XX): wherein P or an acid addition salt thereof; wherein X is a QH or a leaving group, to form a compound of formula (XXIII):