LINCOMYCIN DERIVATIVES AND PROCESS FOR PRODUCING THE SAME

摘要

1,250,558. Lincomycins. UPJOHN CO. 1 Oct., 1969 [17 Oct., 1968], No. 48342/69. Heading C2C. [Also in Division C3] Compounds of Formula I where R is 1-20C alkyl, 3-8C-cycloalkyl, or 7_12C-aralkyl; Ac1 is H or trimethylsilyl (see also Division C3) and Ac is Ac1 or an acyl radical of a 4-substituted-L-2-pyrrolidine=carboxylic acid are prepared by heating a solution of NaCN with a compound (II) where R is as defined above, Ac1 is a protective group and Ac is Ac1 or is an acyl radical of a 4 - substituted - L - 2 - pyrrolidine carboxylic acid, and removing the protective groups by acid hydrolysis. 7(5). Chloro - 7 - deoxylincomycin and methyl 7(S) - chloro - 7 - deoxy - α - thiolincosaminide are prepared as intermediates. Pharmaceutical compositions comprise the compounds of Formula (I) in admixture with a carrier. Compounds (I) have antibacterial properties similar to lincomycin.