Halofantrine hydrochloride, SK&F-102866, WR-171669, Halfan-药物合成数据库

【药物名称】Halofantrine hydrochloride, SK&F-102866, WR-171669, Halfan

化学结构式(Chemical Structure):

参考文献No.	70735
标题:	Halofantrine hydrochloride
作者:	Hillier, K.; Casta馿r, J.; Blancafort, P.; Serradell, M.N.
来源:	Drugs Fut 1980,5(11),547

合成路线图解说明: The reduction of 1,3-dichloro-6-trifluoromethylphenanthrene-9-carboxylic acid (I) with BH3 in THF gives 1,3-dichloro-6-trifluoromethyl-9-hydroxymethylphenanthrene (II), which is oxidized with lead tetracetate in pyridine to yield 1,3-dichloro-6-trifluoromethylphenanthren-9-carboxaldehyde (III). The reaction of (III) with N,N-dibutylbromoacetamide (IV) by means of Zn in THF affords 1,3-dichloro-6-trifluoromethyl-9-[3-(dibutylamino)-3-oxo-1-hydroxypropyl]phenanthrene (V), which is finally reduced with BH3 as before, and treated with HCl.

参考文献No.	84663
标题:	Antimalarial arylaminopropanols
作者:	Colwell, W.T.; et al.
来源:	J Med Chem 1972,15771-775

合成路线图解说明: The reduction of 1,3-dichloro-6-trifluoromethylphenanthrene-9-carboxylic acid (I) with BH3 in THF gives 1,3-dichloro-6-trifluoromethyl-9-hydroxymethylphenanthrene (II), which is oxidized with lead tetracetate in pyridine to yield 1,3-dichloro-6-trifluoromethylphenanthren-9-carboxaldehyde (III). The reaction of (III) with N,N-dibutylbromoacetamide (IV) by means of Zn in THF affords 1,3-dichloro-6-trifluoromethyl-9-[3-(dibutylamino)-3-oxo-1-hydroxypropyl]phenanthrene (V), which is finally reduced with BH3 as before, and treated with HCl.