【药物名称】Mepirodipine hydrochloride, Barnidipine hydrochloride, EU-730, YM-730, YM-09730-5, Cyress, Vasexten, Hypoca
化学结构式(Chemical Structure):
参考文献No.3087
标题:1,4-Dihydropyridine-3,5-dicarboxylic acid ester de
作者:Kojima, T.; Takenaka, T. (Yamanouchi Pharmaceutical Co., Ltd.)
来源:DE 2904552; US 4220649
合成路线图解说明:

By cyclocondensation of 3-nitrobenzaldehyde (I) with methyl 3-aminocrotonate (II) and 1-benzyl-3-(acetoacetoxy)pyrrolidine (III) in refluxing isopropanol. The pyrrolidine (III) is obtained as follows: The condensation of 2-hydroxysuccinic acid (IV) with benzylamine (VI), which is reduced with LiAlH4 in dry THF yielding N-benzyl-3-hydroxypyrrolidine (VIII). Finally, this compound is condensed with diketene (VII) by means of sodium acetate at 80 C.

参考文献No.62085
标题:YM-09730-5
作者:Prous, J.; Casta馿r, J.
来源:Drugs Fut 1988,13(7),634
合成路线图解说明:

By cyclocondensation of 3-nitrobenzaldehyde (I) with methyl 3-aminocrotonate (II) and 1-benzyl-3-(acetoacetoxy)pyrrolidine (III) in refluxing isopropanol. The pyrrolidine (III) is obtained as follows: The condensation of 2-hydroxysuccinic acid (IV) with benzylamine (VI), which is reduced with LiAlH4 in dry THF yielding N-benzyl-3-hydroxypyrrolidine (VIII). Finally, this compound is condensed with diketene (VII) by means of sodium acetate at 80 C.

参考文献No.547123
标题:Synthesis of 14C-and 2H-labeled (3S)-1-benzyl-3-py
作者:Tamazawa, K.; Takeuchi, M.; Arima, H.
来源:J Label Compd Radiopharm 1988,25(2),161
合成路线图解说明:

By cyclocondensation of 3-nitrobenzaldehyde (I) with methyl 3-aminocrotonate (II) and 1-benzyl-3-(acetoacetoxy)pyrrolidine (III) in refluxing isopropanol. The pyrrolidine (III) is obtained as follows: The condensation of 2-hydroxysuccinic acid (IV) with benzylamine (VI), which is reduced with LiAlH4 in dry THF yielding N-benzyl-3-hydroxypyrrolidine (VIII). Finally, this compound is condensed with diketene (VII) by means of sodium acetate at 80 C.

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