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【结 构 式】 
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【分子编号】39354 【品名】 【CA登记号】 |
【 分 子 式 】C13H17N5O5S 【 分 子 量 】355.37468 【元素组成】C 43.94% H 4.82% N 19.71% O 22.51% S 9.02% |
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：(XI)In an alternative procedure, d-nitroarginine methyl ester (VIII) was condensed with sulfonyl chloride (V) giving sulfonamide (IX). The hydrolysis of the ester group of (IX) with LiOH produced carboxylic acid (X). Conversion of (X) to arginine lactam (XI) was effected by treatment with EDC and HOBt. Subsequent opening of the lactam ring of (XI) with sarcosine tert-butyl ester (XII) in the presence of AlMe3 gave rise to dipeptide (XIII). The tert-butyl ester of (XIII) was then cleaved by treatment with trifluoroacetic acid.
| 【1】 Semple, J.E.; et al.; Novel, potent, and selective factor Xa inhibitors featuring a hydrophobic P1-ketoamide moiety. 219th ACS Natl Meet (March 26 2000, San Francisco) 2000, Abst MEDI 193. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (V) | 25151 | phenylmethanesulfonyl chloride | 1939-99-7 | C7H7ClO2S | 详情 | 详情 |
| (VII) | 39350 | C16H24N6O7S | 详情 | 详情 | ||
| (VIII) | 39351 | D-Ornithine, N5-(imino(nitroamino)methyl)-, methyl ester; N5-(Imino(nitroamino)methyl)-D-ornithine methyl ester | 141968-19-6 | C7H15N5O4 | 详情 | 详情 |
| (IX) | 39352 | C14H21N5O6S | 详情 | 详情 | ||
| (X) | 39353 | C13H19N5O6S | 详情 | 详情 | ||
| (XI) | 39354 | C13H17N5O5S | 详情 | 详情 | ||
| (XII) | 39355 | tert-butyl 2-(methylamino)acetate | C7H15NO2 | 详情 | 详情 | |
| (XIII) | 39356 | C20H32N6O7S | 详情 | 详情 |
Extended Information