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【结 构 式】

【药物名称】Dimethylaminoarglabin hydrochloride, Arglabin-DMA.HCl

【化学名称】(3aR,4aS,6aS,9aS,9bR)-7-(Dimethylaminomethyl)-1,4a-dimethyl-5,6,6a,7,9a,9b-hexahydro-3H-oxireno[8,8a]azuleno[4,5-b]furan-8(4aH)-one hydrochloride

【CA登记号】188899-01-6, 215598-04-2 (free base)

【 分 子 式 】C17H26ClNO3

【 分 子 量 】327.85467

【开发单位】Institute of Phytochemistry, Kazakstan (Originator), NuOncology Labs (Originator)

【药理作用】ONCOLYTIC DRUGS, Farnesyl Transferase Inhibitors, Inhibitors of Signal Transduction Pathways

合成路线1

Arglabin (I) was isolated from the extracts of Artemisia glabella and was purified by column chromatography followed by crystallization from hexane. Conjugate addition of dimethylamine to the methylene lactone system of (I) provided the target dimethylamino derivative, which was finally converted to the corresponding hydrochloride salt.

1 Adekenov, S.M. (Paracure, Inc.); Pharmaceutical compsns. of arglabin and arglabin derivs.. US 5902809; WO 9848789 .
2 Shaikenov, T.E. (International Phytochemistry Research Laboratory Ltd.); Farnesyl-protein transferase inhibitors. WO 9943314 .
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) 51405 2-Butynoic acid methyl ester; Methyl 2-butynoate; Tetrolic acid methyl ester; Methyl tetrolate 23326-27-4 C5H6O2 详情 详情
Extended Information