| 摘要 |
<p>1,170,336. Lincomycin-2-acylates and intermediates therefor. UPJOHN CO. 10 March, 1967 [1 April, 1966; 27 July, 1966], No. 11440/67. Heading C2C. Lincomycin-2-acylates (claimed as novel when the acyl group is derived from a C 14-18 aliphatic carboxylic acid) are prepared by condensing lincomycin with an aromatic aldehyde or a vinylog thereof to produce a novel 3,4-O- aralkylidene -, - aralkenylidene - or - heterocyclyl - methylene - lincomycin, tritylating with a trityl halide or substituted trityl halide to form the corresponding novel 7-O-trityl compound, acylating to give the corresponding novel 2-acylate, and removing the protecting groups by mild acid hydrolysis or hydrogenolysis. Acid-addition salts of the intermediates and final products are described. The acylates are derived from hydrocarbon carboxylic acids optionally substituted by halogen, NO 2 , NH 2 , CN, CNS or C 1-8 alkoxy. The novel lincomycin-2-acylates may be made up into anti-bacterial compositions with suitable carriers.</p> |
