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项目整合精选>>>Rokitamycin, TMS-19-Q DS 200, TMS-19Q, Rokicid, Rokital, Ricamycin
Rokitamycin, TMS-19-Q DS 200, TMS-19Q, Rokicid, Rokital, Ricamycin
罗他霉素Chemical Name: 3''-O-Propionylleucomycin A5
CAS No. 74014-51-0
项目整合开发状态: Launched-1986
项目研究机构: Pierre Fabre (Originator), Toyo Jozo (Originator), Formenti (Licensee), ISF (Licensee)
合成路线:Leucomycin A5 (I) is acetylated with acetic anhydride giving the corresponding 2'-O-acetyl derivative (II),which is converted to the 3,9-di-O-trimethylsilyl compound (III) by reaction with trimethylsilyl chloride and pyridine.The reaction of (III) with propionyl chloride and tribenzylamine affords 2'-O-acetyl-17,18-enol-18,3''-di-O-propionyl-3,9-di-O-trimethylsilylleucomycin A5 (IV).
合成路线:Compound (IV) by treatment with K2CO3 in aqueous methanol is converted to 2'-O-acetyl-3''-O-propionylleucomycin A5 (V).Finally,this compound is hydrolyzed partially with acetic acid.
📌 参考资料/链接：
参考文献标题:TMS-19Q
文献作者:Serradell,M.N.; Castar,J.; Burnie,J,Matthews,R.
参考来源:Drugs Fut 1985,10(6),486
📄 详细内容
合成路线:Leucomycin A5 (I) is acetylated with acetic anhydride giving the corresponding 2'-O-acetyl derivative (II),which is converted to the 3,9-di-O-trimethylsilyl compound (III) by reaction with trimethylsilyl chloride and pyridine.The reaction of (III) with propionyl chloride and tribenzylamine affords 2'-O-acetyl-17,18-enol-18,3''-di-O-propionyl-3,9-di-O-trimethylsilylleucomycin A5 (IV).
合成路线:Compound (IV) by treatment with K2CO3 in aqueous methanol is converted to 2'-O-acetyl-3''-O-propionylleucomycin A5 (V).Finally,this compound is hydrolyzed partially with acetic acid.
参考文献标题:Acyl derivatives of 16-membered macrolides.I.Synthesis and biological properties of 3''-O-propionylleucomycin A5 (TMS-19-Q)
文献作者:Sakakibaa,H.; Okekawa,O.; Fujiwara,T.; Otani,M.; Omura,S.
参考来源:J Antibiot 1981,34(8),1001
产品链接: CAS No. 74014-51-0››