|
【结 构 式】 
|
【分子编号】53677 【品名】(2S)-2-{[(2S)-2-({[(2S,4R)-1-(tert-butoxycarbonyl)-4-hydroxypyrrolidinyl]carbonyl}amino)propanoyl]amino}-3-hydroxypropanoic acid 【CA登记号】n/a |
【 分 子 式 】C16H27N3O8 【 分 子 量 】389.4058 【元素组成】C 49.35% H 6.99% N 10.79% O 32.87% |
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：(XXIII)The synthesis of the precursor peptide (XVII) was also reported in solution phase. trans-4-Hydroxy-L-proline (XX) was protected as the N-Boc derivative (XII), which was subsequently activated as the pentafluorophenyl ester (XXI). This was condensed with the dipeptide alanyl-serine (XXII) to furnish the protected tripeptide (XXIII). Acidic cleavage of the Boc protecting group of (XXIII) yielded tripeptide (XXIV).
| 【1】 Kaufman, M.J.; Almarsson, O.; Nerurkar, M.J.; Lynch, J.E.; Karki, S.B.; Cameron, M.; Lieberman, D.R.; Robbins, M.A.; Shi, Y.-J. (Merck & Co., Inc.); Salt form of a conjugate useful in the treatment of prostate cancer. US 6355611; WO 0130804 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (XII) | 16094 | (2S,4R)-1-(tert-butoxycarbonyl)-4-hydroxypyrrolidine-2-carboxylic acid;1-(tert-butoxycarbonyl)-4®-hydroxy-L-proline;(2S,4R)-1-(tert-butoxycarbonyl)-4-hydroxytetrahydro-1H-pyrrole-2-carboxylic acid | 16094 | C10H17NO5 | 详情 | 详情 |
| (XX) | 14489 | (2S,4R)-4-hydroxytetrahydro-1H-pyrrole-2-carboxylic acid; L-Hydroxyproline | 51-35-4 | C5H9NO3 | 详情 | 详情 |
| (XXI) | 53675 | 1-(tert-butyl) 2-(2,3,4,5,6-pentafluorophenyl) (2S,4R)-4-hydroxy-1,2-pyrrolidinedicarboxylate | n/a | C16H16F5NO5 | 详情 | 详情 |
| (XXII) | 53676 | (2S)-2-{[(2S)-2-aminopropanoyl]amino}-3-hydroxypropanoic acid | n/a | C6H12N2O4 | 详情 | 详情 |
| (XXIII) | 53677 | (2S)-2-{[(2S)-2-({[(2S,4R)-1-(tert-butoxycarbonyl)-4-hydroxypyrrolidinyl]carbonyl}amino)propanoyl]amino}-3-hydroxypropanoic acid | n/a | C16H27N3O8 | 详情 | 详情 |
| (XXIV) | 53678 | (2S)-3-hydroxy-2-{[(2S)-2-({[(2S,4R)-4-hydroxypyrrolidinyl]carbonyl}amino)propanoyl]amino}propanoic acid | n/a | C11H19N3O6 | 详情 | 详情 |
Extended Information