Patent ID: 6512114
Filing Date: 2003-01-28
Classification: C07D

Abstract:
A process for the synthesis of a compound of formula I or a pharmaceutically acceptable salt thereof, comprising:(a) heating a first reaction medium, at atmospheric pressure, at about 190Â° C. to about 260Â° C., wherein said first reaction medium comprises from about 1 to about 20 parts by weight of a first solvent per 1 part by weight of tricyclic acid II, and wherein said first solvent is selected from the group consisting of decahydronaphthalene, ethylene glycol, mineral oil, phenyl ether, propylene glycol, and tetrahydronaphthylene,to provide the compound of formula I and Isomidazolam in a ratio of about 6:1;(b) reacting the product of step (a) with a base of formula Mâ€”OR1 wherein M is a cation selected from the group consisting of lithium, sodium, and potassium, and R1 is alkyl, in a second reaction medium to provide the compound of formula I and Isomidazolam in a ratio of about 50:1; and(c) isolating the compound of formula I, wherein the foregoing synthesis is conducted without column chromatography.