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【结 构 式】

【分子编号】31966

【品名】N-(2,4-dimethoxybenzyl)glycine; 2-[(2,4-Dimethoxybenzyl)amino]acetic acid

【CA登记号】

【 分 子 式 】C11H15NO4

【 分 子 量 】225.24444

【元素组成】C 58.66% H 6.71% N 6.22% O 28.41%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(VIII)

The cyclization of anhydride (IV) with N-(2,4-dimethoxybenzyl)glycine (VIII) as before gives 7-fluoro-4-(2,4dimethoxybenzyl)-3,4-dihydro-2H-1,4-benzodiazepin-2,5(1H)-dione (IX), which by a new cyclization with (VII) as before is converted into ethyl-8-fluoro-5-(2,4dimethoxybenzyl)-5,6-dihydro-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate (X). The deprotection of (X) with trifluoroacetic acid yields ethyl-8-fluoro-5,6-dihydro-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate (XI), which is finally methylated with methyl iodide and NaH in DMF.

1 Haefely, W.; Hunkeler, W.; Kyburz, E.; Mohler, H.; Pieri, L.; Polc, P.; Gerecke, M. (F. Hoffmann-La Roche AG); Imidazodiazepine derivatives. EP 0027214; GB 2060632; JP 1156968; US 4316839; US 4346033 .
2 Blancafort, P.; Castaner, J.; Hillier, K.; Serradell, M.N.; RO-15-1788. Drugs Fut 1982, 7, 6, 402.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(IV) 31964 6-Fluoro-2H-3,1-benzoxazine-2,4(1H)-dione; 5-Fluoroisatoic acid anhydride C8H4FNO3 详情 详情
(VII) 11877 Cyanoacetic acid ethyl ester; Ethyl 2-cyanoacetate; Ethyl cyanoacetate; Ethyl isocyanacetate 105-56-6 C5H7NO2 详情 详情
(VIII) 31966 N-(2,4-dimethoxybenzyl)glycine; 2-[(2,4-Dimethoxybenzyl)amino]acetic acid C11H15NO4 详情 详情
(IX) 31967 4-(2,4-dimethoxybenzyl)-7-fluoro-3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione C18H17FN2O4 详情 详情
(X) 31968 Ethyl 5-(2,4-dimethoxybenzyl)-8-fluoro-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate; Ethyl-8-fluoro-5-(2,4dimethoxybenzyl)-5,6-dihydro-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate C23H22FN3O5 详情 详情
(XI) 31969 ethyl 8-fluoro-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate C14H12FN3O3 详情 详情
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