Cericlamine hydrochloride, JO-1017
Chemical Name: (?-3-(3,4-Dichlorophenyl)-2-(dimethylamino)-2-methylpropanol hydrochloride; (?-3,4-Dichloro-beta-(dimethylamino)-beta-methylbenzenepropanol hydrochloride
CAS No. 112922-72-2, 112922-73-3 ((-)-enantiomer), 112922-74-4 ((-)-enantiomer, free base), 112922-76-6 ((+)-enantiomer), 112922-75-5 ((+)-enantiomer, free base), 112922-55-1 (free base), 129162-62-5 (undefined stereoch.)
项目整合开发状态: Phase III
项目研究机构: Jouveinal (Originator), Pfizer (Originator), Merckle (Licensee), UCB (Licensee)
合成路线:The reduction of (?-2-(3,4-dichlorobenzyl)alanine (I) with borane - dimethyl sulfide complex in refluxing THF gives (?-2-amino-3-(3,4-dichlorophenyl)-2-methylpropanol) (II),which is then methylated with formaldehyde in refluxing formic acid.
📌 参考资料/链接：
参考文献标题:Aminoalcohols,process for their preparation and their applications,notable in therapy
文献作者:Aubard,G.; Bure,J.; Calvet,A.P.; Gouret,C.; Grouhel,A.G.; Junien,J.-L.(Institut de Recherche Jouveinal)
参考来源:EP 0237366; FR 2593499; JP 1987190150
📄 详细内容
合成路线:The reduction of (?-2-(3,4-dichlorobenzyl)alanine (I) with borane - dimethyl sulfide complex in refluxing THF gives (?-2-amino-3-(3,4-dichlorophenyl)-2-methylpropanol) (II),which is then methylated with formaldehyde in refluxing formic acid.
参考文献标题:Cericlamine Hydrochloride
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1991,16(4),301