【药物名称】Flumezapine, LY-120363
化学结构式(Chemical Structure):
参考文献No.62612
标题:Flumezapine
作者:Blancafort, P.; Casta馿r, J.; Serradell, M.N.
来源:Drugs Fut 1983,8(2),110
合成路线图解说明:

The condensation of 2,5-difluoronitrobenzene (I) with ethyl 2-amino-5-methylthiophene-3-carboxylate (II) by means of triethylamine in hot DMSO or 2-methoxyethanol giving ethyl 2-(4-fluoro-2-nitroanilino)-5-methylthiophene-3-carboxylate (III), which is reduced with H2 over Pd/C in ethanol to ethyl 2-(4-fluoro-2-aminoanilino)-5-methylthiophene-3-carboxylate (IV). The cyclization of (IV) by means of NaH in DMSO affords 9,10-dihydro-7-fluoro-2-methyl-4H-thieno[2,3b][1,5]benzodiazepin-2-one (V), which is finally condensed with N-methylpiperazine by means of TiCl4 in anisole at 120 C.

参考文献No.607200
标题:Heterooarenobenzodiazepines. 3. 4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics
作者:Chakrabarti, J.K.; Horsman, L.; Hotten, T.M.; Pullar, I.A.; Tupper, D.E.; Wright, F.C.
来源:J Med Chem 1980,23(8),878-884
合成路线图解说明:

The condensation of 2,5-difluoronitrobenzene (I) with ethyl 2-amino-5-methylthiophene-3-carboxylate (II) by means of triethylamine in hot DMSO or 2-methoxyethanol giving ethyl 2-(4-fluoro-2-nitroanilino)-5-methylthiophene-3-carboxylate (III), which is reduced with H2 over Pd/C in ethanol to ethyl 2-(4-fluoro-2-aminoanilino)-5-methylthiophene-3-carboxylate (IV). The cyclization of (IV) by means of NaH in DMSO affords 9,10-dihydro-7-fluoro-2-methyl-4H-thieno[2,3b][1,5]benzodiazepin-2-one (V), which is finally condensed with N-methylpiperazine by means of TiCl4 in anisole at 120 C.

参考文献No.701225
标题:Benzodiazepine derivatives
作者:Chakrabarti, J.K.; Tupper, D.E.
来源:DE 2552403; FR 2292479; GB 1533235; JP 51076296
合成路线图解说明:

The condensation of 2,5-difluoronitrobenzene (I) with ethyl 2-amino-5-methylthiophene-3-carboxylate (II) by means of triethylamine in hot DMSO or 2-methoxyethanol giving ethyl 2-(4-fluoro-2-nitroanilino)-5-methylthiophene-3-carboxylate (III), which is reduced with H2 over Pd/C in ethanol to ethyl 2-(4-fluoro-2-aminoanilino)-5-methylthiophene-3-carboxylate (IV). The cyclization of (IV) by means of NaH in DMSO affords 9,10-dihydro-7-fluoro-2-methyl-4H-thieno[2,3b][1,5]benzodiazepin-2-one (V), which is finally condensed with N-methylpiperazine by means of TiCl4 in anisole at 120 C.

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