Process for selectively acylating immunomycin

C - Chemistry – Metallurgy – 12 – P

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C12P 19/26 (2006.01) C07D 498/18 (2006.01) C12P 17/18 (2006.01)

Patent

CA 2045421

9388P/RJNge 18145 TITLE OF THE INVENTION PROCESS FOR SELECTIVELY ACYLATING IMMUNOMYCIN ABSTRACT OF THE DISCLOSURE Described is a new process for selectively acylating FK-506 type immunosuppressant macrolides, including immunomycin (FK-520), in the C-32 position, under novel conditions utilizing an immobilized lipase enzyme, an acyl donor, and a dry, non-hydroxylic organic solvent. The enzyme is absorbed onto a solid support and the enzyme/support catalyzes the C-32 acylation. The enzyme/support complex can then be filtered from the reaction mixture and, recycled for use.

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