GYKI-32887, RGH-7825
Chemical Name: 8-[N-(2-Azidoethyl)-N-(methylsulfonyl)aminomethyl]-6-methylergol-8-ene maleate; N-(2-Azidoethyl)-N-(8,9-didehydro-6-methylergolin-8-ylmethyl)methanesulfonamide maleate
CAS No. 78463-86-2, 78463-83-9 (free base)
项目整合开发状态: Phase II
项目研究机构: Gedeon Richter (Originator)
合成路线:Elimoclavine (I) obtained by fermentation is first O-mesylated and then the mesyl group in the product (II) displaced by 2-aminoethanol to give the hydroxyethylamino derivative (III).Repeated acylation of (III) with mesyl chloride affords the N,O-dimesylate (IV),which exchanges the O-mesyl group for an azido group on treatment with sodium azide to give the base (VI).Salt formation with maleic acid gives RGH-7825 (1,2).
📌 参考资料/链接：
参考文献标题:Novel ergol-8-ene and ergolin compounds and process for preparing same
文献作者:Mago,N.K.E.; et al.(Gedeon Richter Ltd.)
参考来源:DE 3026271; HU 180467
📄 详细内容
合成路线:Elimoclavine (I) obtained by fermentation is first O-mesylated and then the mesyl group in the product (II) displaced by 2-aminoethanol to give the hydroxyethylamino derivative (III).Repeated acylation of (III) with mesyl chloride affords the N,O-dimesylate (IV),which exchanges the O-mesyl group for an azido group on treatment with sodium azide to give the base (VI).Salt formation with maleic acid gives RGH-7825 (1,2).
参考文献标题:RGH-7825
文献作者:N骻r醖i,M.
参考来源:Drugs Fut 1985,10(9),753
产品链接: CAS No. 78463-86-2››