| 摘要 |
1,160,527. Antibiotics. UPJOHN CO. 20 Sept., 1966 [18 Oct., 1965], No. 41869/66. Headings C2A and C2C. The invention comprises a process for preparing non-N-alkylated pyrrolidines and non-N- alkylated substituted pyrrolidines which consists in the addition of a metabolic inhibitor to a micro-organism fermentation for the production of N-alkylated pyrrolidines and N-alkylated substituted pyrrolidines, the inhibitor being a water-soluble sulphonamide possessing antibacterial properties and a carbonyl reagent for inhibiting glutamic acid decarboxylase. The inhibitors may be sulphanilamide, sulphapyridine, thiocarbohydrazide, semicarbazide, thiosemicarbazide, furoic acid hydrazide, isonicotinic acid hydrazide and hydroxylamine. The inhibitor is preferably added after 24 hours fermentation, in stages, in quantities of less than 5 g./litre and in total of up to 8 g./litre. The process is used for the preparation of (a) lincomycin D (i.e. N-demethyl lincomycin) by cultivating the lincomycin-producing micro-organism Streptomyces lincolnensis var. lincolnensis NRRL 2936 of Specification 976,765; (b) N-demethylcelesticetin by cultivating Streptomyces caelestis NRRL 2418 of Specification 768,971. N-Demethyldesalicetin of Formula III: is produced by hydrolysis of N-demethylcelesticetin of Formula II: in aqueous ethanol at pH 12À2. Salts are formed with inorganic acids, e.g. phosphoric acid, and organic acids, e.g. lactic, maleic, fumaric, pamoic, cholic, palmitic, mucic, camphoric, glutaric, glycollic, phthalic and other acids. |
