文档介绍：l【药物名称】Dapoxetine,LY-210448【化学名】(S)-(+)-N,N-Dimethyl-3-(1-naphthyloxy)-1-phenylpropylamine;(+)-(S)-N,N-Dimethyl-alpha[2-(1-naphthyloxy)ethyl]benzylamine【CAS登记号】119356-77-3,129938-20-1(HCl)【结构式】【分子式】C21-H23-N-O【分子量】【原研厂家】Lilly(Originator),DynogenPharmaceuticals(NotDetermined),Alza(Licensee),PPDGenuPro(Licensee)【作用类别】PreventionofPrematureEjaculation,RENAL-UROLOGICDRUGS,TreatmentofMaleSexualDysfunction,5-HTReuptakeInhibitors【研发状态】PhaseIII【合成情况】〖来源〗pdRadiopharm〖合成路线〗〖标题〗Achiralsynthesisofdapoxetinehydrochloride,aserotoninreuptakeinhibitor,andits14Cisotopomer〖合成方法〗pound,Knoevenagelcondensationofbenzaldehyde(I)withmalonicacid(II)inthepresenceofammoniumacetateproducedthebeta-aminoacid(III).Reductivealkylationoftheaminogroupof(III)withformaldehydeproducedthedimethylamine(IV).Then,Fischeresterificationof(IV)withethanolicHClfurnishedtheintermediateaminoester(V).Aminoester(V)oethylcinnamate(VI).Reductionoftheesterfunctionof(V)providedaminoalcohol(VII).Thesodiumalkoxideof(VII)wasthencoupledwith1-fluoronaphthalene(VIII)toproducetheracemicaminoether,whichwasfinallyresolvedintoenantiomersbymeansoftartaricacid.〖作者〗Wheeler,.;O'Bannon,.〖参考〗Wheeler,.;O'Bannon,.;Achiralsynthesisofdapoxetinehydrochloride,aserotoninreuptakeinhibitor,,31,4,305〖出处〗pdRadiopharm1992,31,(4):305〖来源〗pdRadiopharm〖合成路线〗〖标题〗Achiralsynthesisofdapoxetinehydrochloride,asero