【药物名称】Batabulin sodium, T-67(free acid), Tl-138067(free acid), TL-138067(free acid), T-138067(free acid)
化学结构式(Chemical Structure):
参考文献No.37752
标题:Pentafluorobenzenesulfonamides and analogs
作者:Rosen, T.; Medina, J.C.; Flygare, J.; Shan, B.; Clark, D. (Tularik Inc.)
来源:EP 0896533; JP 2000505459; US 5880151; WO 9730677
合成路线图解说明:

By condensation of pentafluorophenylsulfonyl chloride (I) with 3-fluoro-4-methoxyaniline (II) in pyridine.

合成路线图解说明:

The title sulfonamide was obtained by condensation of pentafluorophenyl sulfonyl chloride (I) with 3-hydroxy-4-methoxyaniline (II) in the presence of pyridine.

合成路线图解说明:

Condensation of pentafluorophenyl sulfonyl chloride (I) with 3-hydroxy-4-methoxyaniline (II) in the presence of pyridine afforded sulfonamide (III). Treatment of (III) with N,N-diisopropyl dibenzylphosphoramidite (A) and tetrazole gave phosphite ester (IV), which was subsequently oxidized to phosphate (V) by means of tert-butyl peroxide. Finally, hydrogenolysis of the benzyl phosphate ester groups of (V) in the presence of Pd/C and 1,4-cyclohexadiene furnished the title compound.

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