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【结 构 式】

【药物名称】EMATE

【化学名称】3-(Sulfamoyloxy)estra-1,3,5(10)-trien-17-one
      Estrone-3-O-sulfamate

【CA登记号】148672-09-7

【 分 子 式 】C18H23NO4S

【 分 子 量 】349.45231

【开发单位】

【药理作用】Cognition Disorders, Treatment of, NEUROLOGIC DRUGS, ONCOLYTIC DRUGS, Estrogen Agonists, Steryl Sulfatase Inhibitors

合成路线1

By esterification of estrone (I) with chlosulfonamide (II) and NaH in DMF.

1 Potter, B.V.L.; Howarth, N.M.; Purohit, A.,; Reed, M.J.; Steroid sulphatase inhibitors: a new endocrine therapy. Drugs Fut 1994, 19, 7, 673.
2 Reed, M.J.; Potter, B.V.L.; Purohit, A.,; Howarth, N.M.; Cooper, G.; Duncan, L.J.; Phosphonates and thiophosphonates as sulfate surrogates: Synthesis of estrone 3-methylthiophosphonate a potent inhibitor of estrone sulfatase. Bioorg Med Chem Lett 1993, 3, 2, 313-318.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 20468 (8R,9S,13S,14S)-3-hydroxy-13-methyl-6,7,8,9,11,12,13,14,15,16-decahydro-17H-cyclopenta[a]phenanthren-17-one 53-16-7 C18H22O2 详情 详情
(II) 40598 amidosulfonoyl chloride 7778-42-9 H2ClNO2S 详情 详情
Extended Information