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【结 构 式】

【分子编号】69304

【品名】5-carbamoyl-5H-dibenzo[b,f]azepin-10-yl acetate

【CA登记号】 

【 分 子 式 】C17H14N2O3

【 分 子 量 】294.30984

【元素组成】C 69.38% H 4.79% N 9.52% O 16.31%

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:(IX)

Alcohol (V) can also be obtained by enantioselective reduction of oxcarbazepine (I) by transfer hydrogenation with formic acid/triethylamine in the presence of the chiral Noyori catalyst [(S,S)-N-tosyl-1,2-diphenylethylenediamino](η6-p-cymene)chlororuthenium .
Alternatively, treatment of oxcarbazepine (I) with acetic anhydride and DMAP in pyridine/CH2Cl2 yields the enol acetate (IX), which is submitted to asymmetric hydrogenation with H2 in the presence of a chiral rhodium(I) catalyst .

3 Yu, B., Li, W., Learmonth, D. (Bial – Portela & Ca., SA). Preparation of eslicarbazepine and related compounds by asymmetric hydrogenation. CA 2648916, EP 2004610, GB 2437078, WO 2007117166.
1 Learmonth, D.A., Grasa, G.A., Zanotti-Gerosa, A. (Bial – Portela & Ca.,SA). Asymmetric catalytic reduction of oxcarbazepine. CA 2616984, EP 1915346, JP 2009502893, WO 2007012793.
2 Mathes, C., Sedelmeier, G., Blatter, F., Pfeffer, S., Grimler, D. (Novartis AG; Novartis Pharma GmbH). Enantioselective process for the preparation of both enantiomers of 10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxamide and new crystal forms thereof. CA 2501237, EP 1551808, JP 2006504710, US 2006142566, WO 2004031155.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 33774 10-oxo-10,11-dihydro-5H-dibenzo[b,f]azepine-5-carboxamide 28721-07-5 C15H12N2O2 详情 详情
(IX) 69304 5-carbamoyl-5H-dibenzo[b,f]azepin-10-yl acetate   C17H14N2O3 详情 详情
Extended Information