新产品编号:628563

Chemical Name: 4-(Diphenylmethyl)-1-[3-phenylprop-2(E)-enyl]-1-(phosphonooxymethyl)piperazin-1-ium trifluoroacetate
CAS No. 243656-14-6, 243656-13-5 (free cation)
项目整合开发状态: Preclinical
项目研究机构: University of Kansas (Originator)
合成路线:Treatment of cinnarizine (I) with phosphate (IV) in acetonitrile in the presence of the proton scavenger 1,2,2,6,6-pentamethylpiperidine affords cinarizinium chloride (II),which is finally treated with TFA in benzene to yield the target trifluoroacetate derivative.Phosphate (IV) can be obtained from phosphite (III) by first treatment with KHCO3 and KMnO4 followed by conversion to tetramethylammonium di-tert-butylphosphate by means of tetramethylammonium hydroxide and final treatment with chloroiodomethane (A) in refluxing dimethoxyethane.

合成路线:Loxapine (I) is treated with phosphate (IV) in acetonitrile in the presence of the proton scavenger 1,2,2,6,6-pentamethylpiperidine to afford loxapinium chloride (II),which is finally treated with TFA in benzene to yield the target trifluoroacetate derivative.Phosphate (IV) can be obtained from phosphite (III) by treatment with KHCO3 and KMnO4 followed by conversion to tetramethylammonium di-tert-butylphosphate by means of tetramethylammonium hydroxide and final treatment with chloroiodomethane (A) in refluxing dimethoxyethane.