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19-DEFORMYL-23-DEMYCINOSYL-23-O-SUBSTITUTED CARBAMOYLDESMYCOSIN DERIVATIVE AND ITS PREPARATION

机译：19-甲酰-23-二甲磺酰基-23-O-取代的羧甲基去氧麦考辛衍生物及其制备

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NEW MATERIAL:The compound of formula I [R1 is (substituted) phenyl; R2 and R3 are H or lower alkyl] and its salt. EXAMPLE:19-Deformyl -23- demycinosyl -23-O-( N-methylbenzylcarbamoyl)-desmycosin. USE:An antibacterial agent, a remedy for infectious diseases of animal, and a feed additive. It has strong antibacterial activity especially against Gram-positive bacteria. PROCESS:The objective compound can be prepared by reacting the compound of formula II (R4 is OH-protecting group) with 1,1'-carbonyldiimidazole in an inert organic solvent (e.g. dichloromethane) at room temperature to convert the 23-OH group to imidazolide, reacting the imidazolide derivative with the amine of formula III (e.g. benzylamine) in an inert organic solvent (e.g. dichloroethane) at about 70-90 deg.C, and heating the reaction product in a lower alcohol (e.g. methanol) to eliminate the OH-protecting group.

机译：新材料：式Ⅰ化合物[R1为（取代）苯基; [R2和R3为H或低级烷基]及其盐。实施例：19-甲酰基-23-去甲糖基-23-O-（N-甲基苄基氨基甲酰基）-脱粘菌素。用途：抗菌剂，动物传染病的治疗剂和饲料添加剂。它具有强大的抗菌活性，尤其是针对革兰氏阳性细菌。过程：目标化合物可以通过在室温下在惰性有机溶剂（例如二氯甲烷）中使式II的化合物（R4为OH-保护基）与1,1'-羰基二咪唑反应，以将23-OH基团转化为咪唑化物，使咪唑化物衍生物与式III的胺（例如苄胺）在惰性有机溶剂（例如二氯乙烷）中于约70-90℃反应，然后在低级醇（例如甲醇）中加热反应产物以消除OH保护基。

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公开/公告号JPS5951298A

专利类型
公开/公告日1984-03-24

原文格式PDF
申请/专利权人 TOYO JOZO KK;
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申请/专利号JP19820157922
发明设计人 FUJIWARA TATSUROU;HIRANO TAKAO;SAKAKIBARA HIDEO;
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申请日1982-09-09
分类号C07H17/08;A61K31/70;A61K31/7042;A61K31/7048;A61P31/04;
国家 JP
入库时间 2022-08-22 09:33:30

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