Batabulin sodium, T-67(free acid), Tl-138067(free acid), TL-138067(free acid), T-138067(free acid)

巴他布林酸钠Chemical Name: 2,3,4,5,6-Pentafluoro-N-(3-fluoro-4-methoxyphenyl)benzenesulfonamide sodium salt
CAS No. 195533-98-3, 195533-53-0 (free acid), 195533-97-2 (K salt), 202998-72-9 (tritium labeled)
项目整合开发状态: Phase III
项目研究机构: Amgen (Originator)
合成路线:By condensation of pentafluorophenylsulfonyl chloride (I) with 3-fluoro-4-methoxyaniline (II) in pyridine.

合成路线: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: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.