【药物名称】SB-238039
化学结构式(Chemical Structure):
参考文献No.32055
标题:Imidazole cpds.
作者:Adams, J.L.; Gallagher, T.F.; Sisko, J.; Peng, Z.-Q.; Osifo, I.K.; Boehm, J.C. (SmithKline Beecham plc)
来源:EP 0831830; JP 1999513017; US 5658903; WO 9640143
合成路线图解说明:

2-Chloronicotinic acid (I) was reduced to alcohol (II) employing borane, generated from NaBH4 and BF3.Et2O. Subsequent oxidation of (II) with N-bromosuccinimide produced aldehyde (III), which was condensed with N-Boc-4-aminopiperidine (IV), yielding imine (V). Addition to (V) of (4-fluorophenyl)-toluenesulfonylmethyl isocyanide (VI) gave rise to imidazole (VII). Then, displacement of the 2-chloro of (VII) by means of aniline (VIII) in the presence of NaH furnished the 2-anilinopyridine derivative (IX). The Boc protecting group of (IX) was finally removed by treatment with trifluoroacetic acid.

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