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32. 发明授权

US4348264A Photocatalyzed process for producing carbapenams and carbapen-2-ems 失效
标题翻译：用于生产碳青霉烯和碳青霉素2-em的光催化过程
公开(公告)号：US4348264A
公开(公告)日：1982-09-07
申请号：US232156
申请日：1981-02-09
申请人： Robert L. Rosati
发明人： Robert L. Rosati
IPC分类号： C07D487/04 , C07D477/26 , C07D499/00 , B01J19/12
CPC分类号： C07D477/26 , C07D499/00 , Y02P20/55
摘要： Carbapenam-3-carboxylic acids and carbapen-2-em-3-carboxylic acids substituted at the 1-position with an oxo, a hydroxy or an acetoxy group, variously substituted at the 2-position with such groups as methyl, acetoxymethyl, methanesulfonyloxy, alkoxy, alkylthio, aminoalkylthio or amidinoalkylthio and optionally substituted at the 6-position with a hydroxyalkyl group, an acetoxyalkyl group or a conventional penicillin side-chain, pharmaceutically-acceptable salts thereof and various esters thereof wherein the esterifying group is selectively removed in the laboratory, or hydrolyzed under physiological conditions.These compounds are useful either systemically or topically in the treatment of diseases caused by susceptible microorganisms, as animal feed additives for promotion of growth, or in the preservation of biodegradable materials, or as intermediates to compounds having such antibacterial activity.Key to the synthesis of these compounds is the light catalyzed rearrangement of 2-diazo-1-oxoceph-3-em-4-carboxylates to 1-oxocarbapen-2-em-3-carboxylates, a newly discovered reaction determined to be of general applicability.
摘要翻译：在1-位被氧代，羟基或乙酰氧基取代的碳青霉烯-3-羧酸和在2-位上被甲基，乙酰氧基甲基，甲磺酰氧基等基团取代的碳代萘-2-羧酸，烷氧基，烷硫基，氨基烷硫基或脒基烷硫基，并且任选在6-位被羟烷基，乙酰氧基烷基或常规青霉素侧链取代，其药学上可接受的盐及其各种酯，其中酯化基团在实验室，或在生理条件下水解。这些化合物可以全身或局部用于治疗由易感微生物引起的疾病，作为用于促进生长的动物饲料添加剂，或用于生物降解材料的保存，或作为具有这种抗菌活性的化合物的中间体。合成这些化合物的关键是2-重氮-1-氧代头孢-3-烯-4-羧酸酯轻链催化重排1-氧代羧基-2-em-3-羧酸酯，新发现的反应确定为一般适用性。

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