Mosapramine hydrochloride, Clospipramine hydrochloride, Y-516, Cremin

合成路线:By condensation of 3-chloro-5-(3-methylsulfonyloxypropyl)-10,11-dihydro-5H-dibenzo[b,f]azepine (I) with 1,2,3,5,6,7,8,8a-octahydroimidazo[1,2-a]pyridine-3-spiro 4'-piperidin-2-one (II) by means of K2CO3 in hot ethanol,and treatment with HCl.

参考文献标题:Y-516
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1987,12(4),365


合成路线:The synthesis of the optical isomers of mosapramine has been reported:A solution of racemic spiro(octahydroimidazo[1,2-a]pyridine-3,4'-piperidin)-2-one (I) with N-acetyl-L-tryptophan in hot isopropanol is allowed to crystallize.The precipitate collected is recrystallized from isopropanol and treated with aqueous NH4OH,extracted with CHCl3,evaporated and crystallized from isopropanol to obtain the R-(-)-enantiomer of (I).The condensation of R-(-)-(I) with 3-chloro-5-[3-(methanesulfonyloxy)propyl]-10,11-dihydro-5H-dibenzo[b,f] azepine (II) by means of triethylamine in refluxing CHCl3 affords the R-(-)-isomer of mosapramine.The mother liquors of the separation of R-(-)-(I) are treated with aqueous NH4OH and extracted with CHCl3.This extract is purified by treatment with N-acetyl-D-tryptophan to obtain S-(+)-(I),which is then condensed with (II) as before,yielding the S-(+)-isomer of mosapramine.
参考文献标题:Chem Pharm Bull
文献作者:Tashiro,C.; Setoguchi,S.; Fukuda,T.; Marubayashi,N.
参考来源:Chem Pharm Bull 1993,41(6),1074


产品链接: CAS No. 89419-40-9››

产品链接: CAS No.98043-60-8››