Estramustine phosphate sodium, Ro-21-8837/001, Estracyt, Emcyt
雌莫司汀磷酸钠 雌莫司汀 Chemical Name: (17beta)-Estra-1,3,5(10)-triene-3,17-diol 3-[bis(2-chloroethyl)carbamate] 17-(dihydrogen phosphate) disodium salt; Estradiol 3-[bis(2-chloroethyl)carbamate] 17-(dihydrogen phosphate) disodium salt
CAS No. 52205-73-9, 2998-57-4 (free acid)
项目整合开发状态: Launched-1980
项目研究机构: Roche (Originator), Nippon Shinyaku (Not Determined), Leo (Licensee), Lundbeck (Licensee), Pfizer (Licensee)
合成路线:Estradiol 3-N-bis(2-chloroethyl)carbamate (IV) was prepared by treatment of estradiol (I) with either the carbamoyl chloride (II) or the carbamoyl bromide (III) in the presence of various bases such as triethylamine and DMAP or DBU.Phosphorylation of (IV) with phosphorus oxychloride and pyridine,followed by aqueous hydrolysis,produced the 17-O-phosphate ester (V).This was converted to the corresponding disodium salt by treatment with sodium methoxide.
📌 参考资料/链接：
参考文献标题:A selective acylation process
文献作者:Stamvik,A.R.; Kristensson,S.K.(Leo Pharma AB)
参考来源:EP 0138153
📄 详细内容
合成路线:Estradiol 3-N-bis(2-chloroethyl)carbamate (IV) was prepared by treatment of estradiol (I) with either the carbamoyl chloride (II) or the carbamoyl bromide (III) in the presence of various bases such as triethylamine and DMAP or DBU.Phosphorylation of (IV) with phosphorus oxychloride and pyridine,followed by aqueous hydrolysis,produced the 17-O-phosphate ester (V).This was converted to the corresponding disodium salt by treatment with sodium methoxide.
参考文献标题:Method for selective acylation of estradiol
文献作者:Ohwaki,K.; Niino,H.
参考来源:EP 0614909
合成路线:Estradiol 3-N-bis(2-chloroethyl)carbamate (IV) was prepared by treatment of estradiol (I) with either the carbamoyl chloride (II) or the carbamoyl bromide (III) in the presence of various bases such as triethylamine and DMAP or DBU.Phosphorylation of (IV) with phosphorus oxychloride and pyridine,followed by aqueous hydrolysis,produced the 17-O-phosphate ester (V).This was converted to the corresponding disodium salt by treatment with sodium methoxide.
参考文献标题:Method for purification of estramustin phosphate or salt thereof
文献作者:Ohwaki,K.; Niino,H.; norose,S.
参考来源:EP 0612760
产品链接: CAS No. 52205-73-9›› 产品链接: CAS No.2998-57-4››