Process for the preparation of derivatives of cyclic peptide...

C - Chemistry – Metallurgy – 07 – K

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530/7.06

C07K 7/56 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1182812

Abstract of the Disclosure Described herein is a process for the preparation of compounds of the formula Image III wherein R1 is H or OH;and when R1 is H, R2 is H and R3 and R4 are both H or both OH, and when R1 is OH, R2 is H, R3 is OH or C1-C6 alkyloxy and R4 is OH, or R2 is -CO-NH2 and R3 and R4 are both OH, and wherein R5 is C6-C24 alkyl or C6-C24 alkenyl, which have antifungal activity. The process comprises acylating with an alkanoic or alkenoic acid a cyclic peptide nucleus of the formula Image II wherein R1 is H or OH; and when R1 is H, R2 is H and R3 and R4 are both H or both OH, and when R1 is OH, R2 is H, R3 is OH or C1-C6 alkyloxy and R4 is OH, or R2 is Image and R3 and R4 are both OH.

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