【药物名称】Clomiphene, Serofene, Clomid(citrate), Serophene(citrate)
化学结构式(Chemical Structure):
参考文献No.900432
标题:
作者:Allen, R.E.; et al.
来源:DE 1155436
合成路线图解说明:

The Grignard reaction of 4-(beta-diethylaminoethoxy)benzophenone (I) with benzylmagnesium chloride (II) yields the diphenyl benzyl carbinol (III), which is dehydrated to the ethylene (IV) by treatment with HCl in refluxing ethanol. The reaction of (IV) first with N-chlorosuccinimide (V) and then with K2CO3 affords a mixture of cis- and trans-1-[p-(beta-diethylaminoethoxy)phenyl]-1,2-diphenylchloroethylene (VI), which by treatment with citric acid (VII) is converted into the corresponding citrate (VIII) (1). Finally this compound is treated with binaphthyl-phosphoric acid (IX) in methanol in order to separate cis and trans isomers (2).

参考文献No.900433
标题:
作者:Viterbo, R.; Jacques, J.
来源:CA 961500; DE 2212660; FR 2129741; GB 1360946; US 3848030; ZA 7201297
合成路线图解说明:

The Grignard reaction of 4-(beta-diethylaminoethoxy)benzophenone (I) with benzylmagnesium chloride (II) yields the diphenyl benzyl carbinol (III), which is dehydrated to the ethylene (IV) by treatment with HCl in refluxing ethanol. The reaction of (IV) first with N-chlorosuccinimide (V) and then with K2CO3 affords a mixture of cis- and trans-1-[p-(beta-diethylaminoethoxy)phenyl]-1,2-diphenylchloroethylene (VI), which by treatment with citric acid (VII) is converted into the corresponding citrate (VIII) (1). Finally this compound is treated with binaphthyl-phosphoric acid (IX) in methanol in order to separate cis and trans isomers (2).

参考文献No.950187
标题:Zuclomiphene
作者:Casta馿r, J.; Paton, D.M.
来源:Drugs Fut 1978,3(11),850
合成路线图解说明:

The Grignard reaction of 4-(beta-diethylaminoethoxy)benzophenone (I) with benzylmagnesium chloride (II) yields the diphenyl benzyl carbinol (III), which is dehydrated to the ethylene (IV) by treatment with HCl in refluxing ethanol. The reaction of (IV) first with N-chlorosuccinimide (V) and then with K2CO3 affords a mixture of cis- and trans-1-[p-(beta-diethylaminoethoxy)phenyl]-1,2-diphenylchloroethylene (VI), which by treatment with citric acid (VII) is converted into the corresponding citrate (VIII) (1). Finally this compound is treated with binaphthyl-phosphoric acid (IX) in methanol in order to separate cis and trans isomers (2).

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