Rimcazole hydrochloride, SH 1/76(monohydrochloride), BW-234U(free base)
林卡唑 9H-卡巴唑,9-[3-[(3R,5S)-3,5-二甲基-1-吡嗪基]丙基]-,rel- 9-[3-(顺式-3,5-二甲基-1-哌嗪基)丙基]咔唑单盐酸盐Chemical Name: cis-9-[3-(3,5-Dimethyl-1-piperazinyl)propyl]-9H-carbazole dihydrochloride
CAS No. 75859-03-9, 75859-04-0 (free base), 75859-05-1 (monohydrochloride)
项目整合开发状态: Phase III
项目研究机构: GlaxoSmithKline (Originator)
合成路线:The reaction of 3-chloropropanol (I) with 2,6-dimethylpiperazine (II) by means of Na2CO3 in refluxing glycol monomethyl ether gives 3-(3,5-dimethyl-1-piperazinyl)propanol (III),which by reaction with refluxing SOCl2 is converted into 3-(3,5-dimethylpiperazinyl)propyl chloride (IV).Finally,this compound is condensed with carbazole (V) by means of NaH in hot DMF; a final treatment with aqueous HCl yields the dihydrochloride.
📌 参考资料/链接：
参考文献标题:Carbazole compounds and medicinal use thereof
文献作者:Harfenist,M.; Jogner,C.T.(Glaxo Wellcome Inc.)
参考来源:DD 147110; EP 0012208; EP 0051321; US 4379160
📄 详细内容
合成路线:The reaction of 3-chloropropanol (I) with 2,6-dimethylpiperazine (II) by means of Na2CO3 in refluxing glycol monomethyl ether gives 3-(3,5-dimethyl-1-piperazinyl)propanol (III),which by reaction with refluxing SOCl2 is converted into 3-(3,5-dimethylpiperazinyl)propyl chloride (IV).Finally,this compound is condensed with carbazole (V) by means of NaH in hot DMF; a final treatment with aqueous HCl yields the dihydrochloride.
参考文献标题:BW-234U
文献作者:Blancafort,P.; Hilier,K.; Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1983,8(4),303