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【结 构 式】

【分子编号】61011

【品名】1-(tert-butoxycarbonyl)-2-indolinecarboxylic acid

【CA登记号】

【 分 子 式 】C14H17NO4

【 分 子 量 】263.29332

【元素组成】C 63.87% H 6.51% N 5.32% O 24.31%

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:(II)

Indoline-2-carboxylic acid (I) is converted into the N-Boc derivative (II) by treatment with Boc2O. Subsequent coupling of (II) with methyl indoline-2-carboxylate (III) by using 2-chloro-1-methylpyridinium iodide (CMPI) provides amide (IV). Hydrolysis of the methyl ester function of (IV) employing LiOH leads to carboxylic acid (V). This is then coupled to N-epsilon-(benzyloxycarbonyl)-lysine methyl ester (VI) in the presence of CMPI to furnish the title compound.

1 Reichert, D.; Kutscher, B.; Bang, H.; Brune, K.; Quinkert, G.; Schaible, H.-G. (Asta Medica AG); Specific immunophilin ligands as antiasthmatics and immunosuppressants. DE 19616509; EP 0896580; JP 2000500776; WO 9741148 .
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) 34308 ethyl (2S)-2,3-dihydro-1H-indole-2-carboxylate C11H13NO2 详情 详情
(II) 61011 1-(tert-butoxycarbonyl)-2-indolinecarboxylic acid C14H17NO4 详情 详情
(III) 61012 methyl 2-indolinecarboxylate C10H11NO2 详情 详情
(IV) 61013 tert-butyl 2-{[2-(methoxycarbonyl)-2,3-dihydro-1H-indol-1-yl]carbonyl}-1-indolinecarboxylate C24H26N2O5 详情 详情
(V) 61014 1-{[1-(tert-butoxycarbonyl)-2,3-dihydro-1H-indol-2-yl]carbonyl}-2-indolinecarboxylic acid C23H24N2O5 详情 详情
(VI) 31069 methyl (2S)-2-amino-6-[[(benzyloxy)carbonyl]amino]hexanoate C15H22N2O4 详情 详情
Extended Information