【药物名称】NC-1300
化学结构式(Chemical Structure):
参考文献No.4207
标题:Benzimidazole derivs. and antiulcer agents contain
作者:Susumu, O.; Masaru, S.; Tomio, Y.; Yutaka, N.; Masatoshi, H. (Nippon Chemiphar Co., Ltd.)
来源:AU 8546409; BE 0903128; CH 665417; DE 3531487; ES 8703142; FR 2569691; GB 2163747; JP 1986060660; JP 1986221175; JP 1986221176; JP 1991223260; JP 1991223261; JP 1991223262; JP 1991227927
合成路线图解说明:

By condensation of pyrrolidine (I) with paraformaldehyde (II) and 4-ethylpropiophenone (III) by means of dry HCl in refluxing ethyl acetate.

合成路线图解说明:

The condensation of 2-(dimethylamino)benzyl chloride (I) with 2-mercaptobenzimidazole (II) by means of NaHCO3 in ethanol gives 2-[2-(dimethylamino)benzylthio]benzimidazole (III), which is then oxidized with m-chloroperbenzoic acid (IV) in CHCl3-methanol.

合成路线图解说明:

The acylation of methylanthranilate (I) with isobutyryl chloride (II) gives 2-isobutyramidobenzoic acid methyl ester (III), which is reduced with LiAlH4 to 2-(isobutylamino)benzyl alcohol (IV). The methylation of (IV) with dimethyl sulfate yields 2-(N-isobutyl-N-methylamino)benzyl alcohol (V), which is treated with SOCl2 to afford the corresponding benzyl chloride (VI). The condensation of (VI) with benzimidazole-2-thiol (VII) by means of NaOH yields 2-[2-(N-isobutyl-N-methylamino)benzylsulfanyl)benzimidazole (VIII), which is finally oxidized with m-chloroperbenzoic acid (MCPBA) as usual.

参考文献No.54749
标题:NC-1300
作者:Casta馿r, J.; Prous, J.
来源:Drugs Fut 1987,12(1),34
合成路线图解说明:

The condensation of 2-(dimethylamino)benzyl chloride (I) with 2-mercaptobenzimidazole (II) by means of NaHCO3 in ethanol gives 2-[2-(dimethylamino)benzylthio]benzimidazole (III), which is then oxidized with m-chloroperbenzoic acid (IV) in CHCl3-methanol.

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