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【结 构 式】

【分子编号】19048

【品名】methyl (2S)-2-amino-5-[(imino[[(4-methylphenyl)sulfonyl]amino]methyl)amino]pentanoate

【CA登记号】

【 分 子 式 】C14H22N4O4S

【 分 子 量 】342.41924

【元素组成】C 49.11% H 6.48% N 16.36% O 18.69% S 9.36%

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:(VI)

In a solid phase synthesizer, an a-Boc-omega-Ts-Arg-phenylacetamidomethyl resin (V) was treated with trifluoroacetic acid (TFA) in anisole and dichloromethane in order to remove the Boc protecting group, and the resulting (VI) was coupled with Boc-octahydroindolecarboxylic acid (VII) in the presence of diisopropyl carbodiimide (DIPCDI) to give the dipeptide resin (VIII). This was submitted to successive coupling cycles (deprotection with TFA, and coupling with DIPCDI) to introduce sequentially the following amino acids: Boc-D-4-propoxyproline (IV), Boc-Ser(Bzl) (XIa) to yield the following resins: (IXa),(IXb) and (X), respectively.

1 Kyle, D.J.; Hiner, R.N. (Scios Inc.); Bradykinin antagonist peptides. JP 1995504155; US 5385889 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(XIa) 16886 (2S)-3-(benzyloxy)-2-[(tert-butoxycarbonyl)amino]propionic acid; N-alpha-t-BOC-o-benzyl-L-serine 23680-31-1 C15H21NO5 详情 详情
(IXa) 19051 methyl (2S)-2-[[(2S,3aS,7aS)octahydro-1H-indol-2-ylcarbonyl]amino]-5-[(imino[[(4-methylphenyl)sulfonyl]amino]methyl)amino]pentanoate C23H35N5O5S 详情 详情
(IXb) 19052 methyl (2S)-2-[[((2S,3aS,7aS)-1-[[(2R,4S)-4-propoxypyrrolidinyl]carbonyl]octahydro-1H-indol-2-yl)carbonyl]amino]-5-[(imino[[(4-methylphenyl)sulfonyl]amino]methyl)amino]pentanoate C31H48N6O7S 详情 详情
(IV) 19046 (2R,4S)-1-(tert-butoxycarbonyl)-4-propoxy-2-pyrrolidinecarboxylic acid C13H23NO5 详情 详情
(V) 19047 methyl (2S)-2-[(tert-butoxycarbonyl)amino]-5-[(imino[[(4-methylphenyl)sulfonyl]amino]methyl)amino]pentanoate C19H30N4O6S 详情 详情
(VI) 19048 methyl (2S)-2-amino-5-[(imino[[(4-methylphenyl)sulfonyl]amino]methyl)amino]pentanoate C14H22N4O4S 详情 详情
(VII) 19049 (2S,3aS,7aS)-1-(tert-butoxycarbonyl)octahydro-1H-indole-2-carboxylic acid C14H23NO4 详情 详情
(VIII) 19050 tert-butyl (2S,3aS,7aS)-2-([[(1S)-4-[(imino[[(4-methylphenyl)sulfonyl]amino]methyl)amino]-1-(methoxycarbonyl)butyl]amino]carbonyl)octahydro-1H-indole-1-carboxylate C28H43N5O7S 详情 详情
(X) 19053 methyl (2S)-2-([[(2S,3aS,7aS)-1-([(2R,4S)-1-[(2S)-2-amino-3-(benzyloxy)propanoyl]-4-propoxypyrrolidinyl]carbonyl)octahydro-1H-indol-2-yl]carbonyl]amino)-5-[(imino[[(4-methylphenyl)sulfonyl]amino]methyl)amino]pentanoate C41H59N7O9S 详情 详情
Extended Information