首页> 外国专利> METHOD FOR PREPARING OF N, N- DIMETHYLACETAMIDE ADUCT D (-)- ALPHA- (4- ETHYL- 2, 3- DIOXOPYPERAZYNIL) CARBOXAMIDO- ALPHA- (4- HYDROXYPHENYL) ACETAMID- 3- 5- (1- METHYL-

METHOD FOR PREPARING OF N, N- DIMETHYLACETAMIDE ADUCT D (-)- ALPHA- (4- ETHYL- 2, 3- DIOXOPYPERAZYNIL) CARBOXAMIDO- ALPHA- (4- HYDROXYPHENYL) ACETAMID- 3- 5- (1- METHYL-

机译:N,N-二甲基乙酰胺基D-(-)-α-(4-乙基-2-,3-二氧过氧苯乙腈)羧酰胺基-α-(4-羟基苯甲酰基)乙酰胺-3-5-(1-甲基-

摘要

The compound obtained by this method is used in medicine for the preparation of a broad spectrum of parenteral antibiotics. The method is technically simplified and the product is obtained at higher yields, with respect to the raw materials. The method involves adding a suspension of diketopiperazine carbonyl chloride and triethyl amine hydrochloride in anhydrous organic solvent to p-hydroxyphenyl glycine after silylating the latter in a medium of the same solvent. The resulting 2-[(N-ethyl-2,3-dioxo-piperazinyl)carboxamido]-2-(p- hydroxyphenyl)-acetic acid is isolated and after activation with chlorine agents, is reacted with a sylilic derivative of 7-amino-3-/-5-(1-methyl)-1,2,3,4-tetrazolyl) thiomethyl/-cephalosporanic acid in a medium of dimethyl acetamide.
机译:通过该方法获得的化合物在医学上用于制备广泛的肠胃外抗生素。相对于原材料,该方法在技术上得到了简化,并且以更高的收率获得了产品。该方法包括将二酮哌嗪羰基氯和三乙胺盐酸盐在无水有机溶剂中的悬浮液在对-羟基苯基甘氨酸在相同溶剂的介质中甲硅烷基化后添加。分离出所得的2-[((N-乙基-2,3-二氧-哌嗪基)羧酰胺基] -2-(对羟基苯基)-乙酸,并在用氯试剂活化后,使其与7-氨基的甲硅烷基衍生物反应。在二甲基乙酰胺介质中的-3-/-5-(1-甲基)-1,2,3,4-四唑基)硫代甲基/头孢烷酸。

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