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【结 构 式】

【分子编号】20419

【品名】Spiro[indene-1,4'-piperidine]

【CA登记号】

【 分 子 式 】C13H15N

【 分 子 量 】185.26884

【元素组成】C 84.28% H 8.16% N 7.56%

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:(XIV)

Treatment of D-tryptophan methyl ester (XI) with N,N'-disuccinimidyl carbonate (XII) gave the intermediate succinimidyl carbamate (XIII), which was subsequently converted to urea (XV) upon reaction with spiro(indene-1,4'-piperidine) (XIV). Saponification of the ester function of (XV) with LiOH afforded the carboxylic acid (XVI), and this was then coupled with the Boc-protected chiral diamine (X) using EDC and HOBt. The resulting precursor (XVII) was finally deprotected with HCl in EtOAc to provide the title compound.

1 Yang, L.; et al.; Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists. J Med Chem 1998, 41, 13, 2175.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(X) 20415 tert-butyl [(1S,3R)-3-(aminomethyl)cyclohexyl]methylcarbamate C13H26N2O2 详情 详情
(XI) 20416 methyl (2R)-2-amino-3-(1H-indol-3-yl)propanoate C12H14N2O2 详情 详情
(XII) 20417 1-([[(2,5-dioxo-1-pyrrolidinyl)oxy]carbonyl]oxy)-2,5-pyrrolidinedione 74124-79-1 C9H8N2O7 详情 详情
(XIII) 20418 methyl (2R)-2-([[(2,5-dioxo-1-pyrrolidinyl)oxy]carbonyl]amino)-3-(1H-indol-3-yl)propanoate C17H17N3O6 详情 详情
(XIV) 20419 Spiro[indene-1,4'-piperidine] C13H15N 详情 详情
(XV) 20420 N-[Spiro[indene-1,4'-piperidin]-1'-ylcarbonyl]-D-tryptophan methyl ester C26H27N3O3 详情 详情
(XVI) 20421 N-[Spiro[indene-1,4'-piperidin]-1'-ylcarbonyl]-D-tryptophan C25H25N3O3 详情 详情
(XVII) 20422 N-[3(R)-[N-alpha-[Spiro[indene-1,4'-piperidin]-1'-ylcarbonyl]-D-tryptophanamidomethyl]cyclohex-1(S)-ylmethyl]carbamic acid tert-butyl ester C38H49N5O4 详情 详情
Extended Information