CAS: 154-21-2; (2S,4R)-N-((1R,2R)-2-Hydroxy-1-((2R,3R,4S,5R,6R)-3,4,5-Trihydroxy-6-(Methylthio)Tetrahydro-2H-Pyran-2-yl)Propyl)-1-Methyl-4-Propylpyrrolidine-2-Carboxamide

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CAS号13380-36-4 (trans)-4-Propy... | CAS号14810-93-6 Methyl 6-amino-... | CAS号13380-37-5 (2S,4R)-1-methy...

盐酸林可霉素置于吡啶,偶氮二甲酸二异丙酯,Potassium Carbonate,溶剂黄146,三苯基膦体系中,用 甲醇,甲苯 用作溶剂,化学反应 66.0H,反应生成林可霉素
参考文献:盐酸克林霉素杂质的制备方法
标题:盐酸克林霉素杂质的制备方法
摘要:本发明涉及盐酸克林霉素杂质的制备方法,属于药物领域.本发明所要解决的技术问题是现有技术中缺乏高效制备盐酸克林霉素杂质7‑差向林可霉素和7‑差向盐酸克林霉素对照品的方法.本发明提供了式ⅱ所示盐酸克林霉素杂质中间体的制备方法:以式ⅰ所示化合物和r1Cooh为原料,经mitsunobu取代反应制备得到,反应液中添加了胺和/或含氮芳香杂环化合物.本发明还进一步提供了7‑差向林可霉素和7‑差向盐酸克林霉素的完整合成方法:以林可霉素为原料,经过上硅保护基,选择性脱保护,Mitsunobu取代反应,水解反应得7‑差向林可霉素,进一步氯代反应制备得到7‑差向盐酸克林霉素.

专利信息

专利号:US-7361743-B2
优先权日:2004-02-11
标 题 :Lincomycin derivatives possessing antibacterial activity
发明人：LEWIS JASON G; ANANDAN SAMPATH K; O'DOWD HARDWIN; GORDEEV MIKHAIL F; LI LIANSHENG
权利人:PFIZER
摘要:Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. The compounds of the subject invention may exhibit potent activities against bacteria, including Gram positive organisms, and may be useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.