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【结 构 式】

【分子编号】13432

【品名】2-[(E)-(1-Benzyl-4-piperidinyl)methylidene]-5,6-dimethoxy-1-indanone

【CA登记号】120014-07-5

【 分 子 式 】C24H27NO3

【 分 子 量 】377.48332

【元素组成】C 76.36% H 7.21% N 3.71% O 12.72%

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:(III)

The condensation of 5,6-dimethoxy-1-indanone (I) with 1-benzylpiperidine-4-carboxaldehyde (II) by means of butyllithium and diisopropylamine in THF gives 1-benzyl-4-(5,6-dimethoxy-1-oxoindan-2-ylidenemethyl)piperidine (III), which is reduced with H2 over Pd/C in THF and treated with HCl in dichloromethane - ethyl acetate.

1 Sugimoto, H.; Tsuchiya, Y.; Higurashi, K.; Karibe, N.; Iimura, Y.; Sasaki, A.; Yamanashi, Y.; Ogura, H.; Araki, S.; Kosasa, T.; Kusota, A.; Kozasa, M.; Yamatsu, K. (Eisai Co., Ltd.); Cyclic amine cpd., its use and pharmaceutical compsns. comprising it. AU 8818216; EP 0296560; EP 0673927; EP 0742207; JP 1989079151; JP 1998067739; US 4895841; US 5100901 .
2 Sugimoto, H.; Mishima, M.; Iimura, Y.; Synthesis of 1-benzyl-4-[(5,6-dimethoxy[2-14C]-1-indanon)-2-yl]methylpiperidine hydrochloride (E-2020-14C). J Label Compd Radiopharm 1989, 27, 7, 835-9.
3 Castaner, J.; Prous, J.; E-2020. Drugs Fut 1991, 16, 1, 16.
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) 13430 5,6-Dimethoxy-1-indanone; 2,3-Dihydro-5,6-dimethoxy-1H-inden-1-one 2107-69-9 C11H12O3 详情 详情
(II) 13431 1-Benzyl-4-piperidinecarbaldehyde C13H17NO 详情 详情
(III) 13432 2-[(E)-(1-Benzyl-4-piperidinyl)methylidene]-5,6-dimethoxy-1-indanone 120014-07-5 C24H27NO3 详情 详情
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