Patent ID: 8492547
Filing Date: 2013-07-23
Classification: C07D

Abstract:
1. A method for enriching buprenorphine relative to 2-[17-(but-3-enyl)-4,5α-epoxy-3-hydroxy-6-methoxy-6α,14-ethano-14α-morphinan-7α-yl]-3,3-dimethylbutan-2-ol and 17-(cyclopropylmethyl)-α-(1,1-dimethylethyl)-4,5-epoxy-3-hydroxy-6-methoxy-α-methyl-6,14-ethenomorphinan-7-methanol in a buprenorphine product, the method comprising: a. forming a first feed solution by dissolving a crude buprenorphine composition comprising buprenorphine, 2-[17-(but-3-enyl)-4,5α-epoxy-3-hydroxy-6-methoxy-6α,14-ethano-14α-morphinan-7α-yl]-3,3-dimethylbutan-2-ol, and 17-(cyclopropylmethyl)-α-(1,1-dimethylethyl)-4,5-epoxy-3-hydroxy-6-methoxy-α-methyl-6,14-ethenomorphinan-7-methanol in a solvent mixture comprising an acid, a first organic polar solvent, and water; b. contacting the first feed solution with a stationary phase; c. introducing into the stationary phase a first mobile phase comprising a second organic solvent and water, wherein the amount of the second organic solvent is at least 85% (V/V) of the mobile phase; and, d. eluting from the stationary phase a first product fraction comprising between about 80% and 100% of the amount of buprenorphine contained in the crude buprenorphine composition.