【药物名称】Ro-09-3024
化学结构式(Chemical Structure):
参考文献No.585848
标题:Synthesis and structure-activity relationships of novel fungal chitin synthase inhibitors
作者:Masabuchi, K.; Taniguchi, M.; Umeda, I.; Hattori, K.; Suda, H.; Kohchi, Y.; Isshiki, Y.; Sakai, T.; Kohchi, M.; Shirai, M.; Okabe, H.; Sudoh, M.; Yamazaki, T.; Shimma, N.
来源:Bioorg Med Chem Lett 2000,10(13),1459
合成路线图解说明:

The Wittig reaction of 2,6-dinitrobenzaldehyde (I) with (ethoxycarbonylmethylene)triphenylphosphorane (A) produced methyl 2,6-dinitrocinnamate (II). Hydrogenation of the nitro groups and the olefinic double bond of (II) with concomitant cyclization furnished the tetrahydroquinolinone (III). Reductive alkylation of (III) with 6,6-dimethylheptadiynal (IV) and sodium cyanoborohydride produced the secondary amine (V). Finally, the N-methyl group was introduced by a second reductive alkylation with formaldehyde.

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