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【结 构 式】 
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【分子编号】65169 【品名】(2R,3R)-3-methoxy-2-methyl-N-phenethyl-3-[(2S)pyrrolidinyl]propanamide 【CA登记号】 |
【 分 子 式 】C17H26N2O2 【 分 子 量 】290.40572 【元素组成】C 70.31% H 9.02% N 9.65% O 11.02% |
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：2) The reaction of 3(R)-[1-(tert-butoxycarbonyl)-2(S)-pyrrolidinyl]-3-methoxy-2(R)-methylpropionic acid (XXI) with 2-phenylethylamine (VIII) by means of DEPC in dichloromethane gives the amide (XXII), which is deprotected with trifluoroacetic acid to yield the amide (XXIII). Finally, this compound is condensed with the previously described intermediate (VI) by means of DEPC in dichloromethane.
| 【1】 Hamel, E.; Williams, M.D.; Srirangam, J.K.; Chapuis, J.-C.; Durkin, K.P.M.; Barkoczy, J.; Schmidt, J.M.; Bai, R.; Boyd, M.R.; Pettit, G.R.; Antineoplastic agents 337. Synthesis of dolastatin. Anti-Cancer Drug Des 1995, 10, 7, 529. |
| 【2】 Castañer, J.; Leeson, P.; Hoshi, A.; TZT-1027. Drugs Fut 1999, 24, 4, 404. |
| 【3】 Petit, G.R.; Barkoczy, J. (Arizona State University); The elucidation and synthesis of antineoplastic te. EP 0600745; JP 1995002894 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 65169 | (2R,3R)-3-methoxy-2-methyl-N-phenethyl-3-[(2S)pyrrolidinyl]propanamide | C17H26N2O2 | 详情 | 详情 | ||
| (VI) | 23505 | (3R,4S,5S)-4-[((2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-3-methylbutanoyl)(methyl)amino]-3-methoxy-5-methylheptanoic acid | C22H43N3O5 | 详情 | 详情 | |
| (VIII) | 18333 | Phenethylamine; 2-Phenyl-1-ethanamine | 64-04-0 | C8H11N | 详情 | 详情 |
| (XXI) | 23520 | (2R,3R)-3-[(2S)-1-(tert-butoxycarbonyl)pyrrolidinyl]-3-methoxy-2-methylpropionic acid | C14H25NO5 | 详情 | 详情 | |
| (XXII) | 23521 | tert-butyl (2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-(phenethylamino)propyl]-1-pyrrolidinecarboxylate | C22H34N2O4 | 详情 | 详情 |
Extended Information