合成路线: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.
参考文献标题:Cytoprotective agents for stomach and intestine
文献作者:Okabe,S.; Sato,M.; Yamakawa,T.; Nomura,T.; Hayashi,M.(Nippon Chemiphar Co.,Ltd.)
参考来源:JP 1988230633
合成路线: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.
参考文献标题:Method for the preparation of benzimidazole cpds
文献作者:Mazaki,M.; Yamakawa,T.; Nomura,Y.(Nippon Chemiphar Co.,Ltd.)
参考来源:JP 1990078665
合成路线: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.
参考文献标题:Leminoprazole
文献作者:Mealy,N.; Castar,J.
参考来源:Drugs Fut 1996,21(2),155
产品链接: CAS No. 104340-86-5››