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US 5,210,030 AGranted
Process for selectively acylating immunomycin
AssigneeMerck & Co., Inc.
InventorsBrian R. Petuch, Shieh-shung T. Chen, Byron H. Arison
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Abstract
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.
Claims3
A process for selectively acylating the C-32 position in a macrolide which comprises:
- (a) contacting a macrolide which is a member selected from the group consisting of FK-506, FK-520, FK-523 and FK-525,
- (b) with an acyl donor which is a member selected from the group consisting of acetic anhydride, propionic anhydride, butyric anhydride, trifluoroacetic anhydride and mixtures thereof,
- (c) in the presence of fungal AMANO lipase N enzyme immobilized on a solid support,
- (d) in an inert, dry organic solvent which is a member selected from the group consisting of aromatic hydrocarbons, linear ethers, branched ethers, halogenated paraffins, and lower carboxylic acid esters,
- (e) at a temperature range of 10.degree. to 50.degree. C.,
- (f) for a period of time sufficient to obtain said C-32 acylated product;
- and,
- (g) recovering said C-32 acylated product.
5 more elements
Dependencies are inferred from the claim text.