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【结 构 式】

【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