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【结 构 式】 
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【分子编号】57856 【品名】tert-butyl (1S)-1-{[(2S)-2-(aminocarbonyl)pyrrolidinyl]carbonyl}-2,2-dimethylpropylcarbamate 【CA登记号】 |
【 分 子 式 】C16H29N3O4 【 分 子 量 】327.42408 【元素组成】C 58.69% H 8.93% N 12.83% O 19.55% |
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：(III)The condensation of N-(tert-butoxycarbonyl)-L-tert-butyl-glycine N-succinimidyl ester (I) with L-prolinamide (II) by means of DIEA in dichloromethane gives the dipeptide amide (III), which is dehydrated by means of POCl3 and imidazole in pyridine to yield N-(tert-butoxycarbonyl)-L-tert-butylglycyl-L-prolinenitrile (IV). Finally, this compound is deprotected by means of trifluoroacetic acid to provide the target dipeptide nitrile.
| 【1】 Ashworth, D.M.; et al.; 2-Cyanopyrrolidides as potent, stable inhibitors of dipeptidyl peptidase IV. Bioorg Med Chem Lett 1996, 6, 10, 1163. |
| 【2】 Broqua, P. (Ferring BV Group Holding); Compsns. for improving fertility. WO 0056296 . |
| 【3】 Broqua, P. (Ferring BV Group Holding); Compsns. for promoting growth. WO 0056297 . |
| 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) | 57855 | tert-butyl (1S)-1-{[(2,5-dioxo-1-pyrrolidinyl)oxy]carbonyl}-2,2-dimethylpropylcarbamate | C15H24N2O6 | 详情 | 详情 | |
| (II) | 36137 | (2S)-2-pyrrolidinecarboxamide;L-prolinamide | 7531-52-4 | C5H10N2O | 详情 | 详情 |
| (III) | 57856 | tert-butyl (1S)-1-{[(2S)-2-(aminocarbonyl)pyrrolidinyl]carbonyl}-2,2-dimethylpropylcarbamate | C16H29N3O4 | 详情 | 详情 | |
| (IV) | 57857 | tert-butyl (1S)-1-{[(2S)-2-cyanopyrrolidinyl]carbonyl}-2,2-dimethylpropylcarbamate | C16H27N3O3 | 详情 | 详情 |
Extended Information