【药物名称】DR-4365
化学结构式(Chemical Structure):
参考文献No.39900
标题:Tetrahydrobenzindole derivs.
作者:Koyama, M.; Okuno, M.; Hiranuma, T.; Ando, T.; Fuji, K.; Ushiroda, O.; Kikuchi, C.; Shiiyama, M.; Satoh, E. (Meiji Seika Kaisha, Ltd.)
来源:EP 1057814; JP 1999189585; US 6498251; WO 9933804
合成路线图解说明:

Intermediate (III) is prepared by the following route. Acylation of 2-Boc-tetrahydropyridoindole (I) with dimethylcarbamoyl chloride provides the 9-carbamoyl derivative (II). Subsequent Boc group cleavage under acidic conditions furnishes amine (III).

合成路线图解说明:

Tetrahydrobenzo[cd]indol-2-one (IV) is selectively alkylated at position 2a with 1,4-dibromobutane (V) in the presence of NaH to provide the bromobutyl derivative (VI). Then, condensation of bromide (VI) with amine (III) employing K2CO3 in DMF leads to the title compound.

参考文献No.669064
标题:2a-[4-(Tetrahydropyridondol-2-yl)butyl]tetrahydrobenzindole derivatives: New selective antagonists of the 5-hydroxytryptamine7 receptor
作者:Kikuchi, C.; Ando, T.; Watanabe, T.; Nagaso, H.; Okuno, M.; Hiranuma, T.; Koyama, M.
来源:J Med Chem 2002,45(11),2197
合成路线图解说明:

Tetrahydrobenzo[cd]indol-2-one (IV) is selectively alkylated at position 2a with 1,4-dibromobutane (V) in the presence of NaH to provide the bromobutyl derivative (VI). Then, condensation of bromide (VI) with amine (III) employing K2CO3 in DMF leads to the title compound.

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