Patent ID: 6403793
Filing Date: 2002-06-11
Classification: C07D

Abstract:
A process for the preparation of a compound of the formula: which comprises:(1) contacting a compound of the formula: with an oxidizing agent which is osmium tetroxide/N-methyl morpholine to give a compound of the formula: (2) activating the compound from step 1 with an activating agent which is methanesulfonyl chloride and contacting the activated compound with ethanolamine to give a compound of the formula: (3) condensing the compound from step 2 with glyoxal and 4-fluoroboronic acid to give a compound of the formula: (4) intramolecular coupling of the compound from step 3 to give a compound of the formula: (5) quarternizing the amino group of the compound from step 4 to give a compound of the formula: (wherein Xâˆ’ is a counterion)(6) hydrolysis of the compound from step 5 to give a compound of the formula: and (7) hydrogenation of the compound from step 6 to give the compound of the formula: