【药物名称】Mefloquine hydrochloride, WR-142490, Mephaquin, Lariam, Fansimef
化学结构式(Chemical Structure):
参考文献No.53446
标题:Mefloquine
作者:Casta馿r, J.; Playle, A.C.
来源:Drugs Fut 1976,1(6),296
合成路线图解说明:

The PPA condensation of 2-trifluoromethylaniline (I) with ethyl 4,4,4-trifluoroacetoacetate (II) yields 2,8-bis(trifluoromethyl)-4-quinolone (III), which is converted into 2,8-bistrifluoromethyl-4-bromoquinoline (IV) with POBr3. The carboxylation of the quinoline (IV) with butyllithium and CO2 gives 2,8-bistrifluoromethylquinoline-4-carboxylic acid (V); this product is condensed with 2-pyridyllithium (A) giving 2,8-bis(trifluoromethyl)-4-quinolinyl-2-pyridyl ketone (VI). The last step is the reduction of ketone (VI) with H2 over Pt in ethanol.

参考文献No.607658
标题:Antimalarials 7-Bis-(trifluoromethyl)-(2-piperidyl)-4-quinoline methanols
作者:Ohnmacht, C.J.; Patel, A.R.; Lutz, R.
来源:J Med Chem 1971,14(10),926-928
合成路线图解说明:

The PPA condensation of 2-trifluoromethylaniline (I) with ethyl 4,4,4-trifluoroacetoacetate (II) yields 2,8-bis(trifluoromethyl)-4-quinolone (III), which is converted into 2,8-bistrifluoromethyl-4-bromoquinoline (IV) with POBr3. The carboxylation of the quinoline (IV) with butyllithium and CO2 gives 2,8-bistrifluoromethylquinoline-4-carboxylic acid (V); this product is condensed with 2-pyridyllithium (A) giving 2,8-bis(trifluoromethyl)-4-quinolinyl-2-pyridyl ketone (VI). The last step is the reduction of ketone (VI) with H2 over Pt in ethanol.

参考文献No.607986
标题:Optical isomers of aryl-2-piperidylmethanol antimalarial agents. Preparation, opticol purity and absolute stereochemistry
作者:Carrol, F.I.; Blackwell, J.T.
来源:J Med Chem 1974,17(2),210-219
合成路线图解说明:

The PPA condensation of 2-trifluoromethylaniline (I) with ethyl 4,4,4-trifluoroacetoacetate (II) yields 2,8-bis(trifluoromethyl)-4-quinolone (III), which is converted into 2,8-bistrifluoromethyl-4-bromoquinoline (IV) with POBr3. The carboxylation of the quinoline (IV) with butyllithium and CO2 gives 2,8-bistrifluoromethylquinoline-4-carboxylic acid (V); this product is condensed with 2-pyridyllithium (A) giving 2,8-bis(trifluoromethyl)-4-quinolinyl-2-pyridyl ketone (VI). The last step is the reduction of ketone (VI) with H2 over Pt in ethanol.

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