Process for the Preparation of Bortezomib Mannitol Ester

摘要

A novel and improved process for preparation of bortezomib mannitol ester is derived, which process avoids excessive use of solvents, involves convenient, industrially feasible and economical techniques, and provides improvements in purity over processes known in the art.

主权项

1. A process for the preparation of bortezomib-mannitol ester (compound B),comprising:
(a) dissolving bortezomib (compound A)  in a first solvent to form a first solution; (b) adding mannitol to the first solution; (c) removing the first solvent from the first solution to form a residue comprising bortezomib-mannitol ester; (d) adding a second solvent to the residue to form a suspension of bortezomib-mannitol ester in the second solvent; and (e) isolating the bortezomib-mannitol ester from the second solvent.