C-31 methylated FR-900520 cyclic hemiketal immunosuppressant agents,申请号US19910738995-传众专利搜索

C-31 methylated FR-900520 cyclic hemiketal immunosuppressant agents

申请公布号：US5149701(A)

申请号：US19910738995

申请日期：1991.08.01

申请公布日期：1992.09.22

申请人：

MERCK & CO., INC.

发明人：SHAFIEE, ALI;KAPLAN, LOUIS;CHEN, SHIEH-SHUNG T.;ARISON, BYRON H.;COLWELL, JR., LAWRENCE F.;DUMONT, FRANCIS

分类号：C07D498/22

主分类号：C07D498/22

摘要：Described is a process for producing a new immunosuppressant, a C-31 desmethyl, C-19/C-22 cyclic hemiketal biotransformation analog (Compound I) of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces, lavendulae ATCC No. 55209. Also disclosed is the C-31 methylated devivative (Compound II) of Compound I produced by enzymatic methylation using 31-O-desmethylimmunomycin O-methyl transferase, (DIMT), a methyl transferase enzyme. The macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.