【结 构 式】 |
【分子编号】41580 【品名】4-(bromomethyl)-N,N-dimethylaniline; N-[4-(bromomethyl)phenyl]-N,N-dimethylamine 【CA登记号】 |
【 分 子 式 】C9H12BrN 【 分 子 量 】214.10502 【元素组成】C 50.49% H 5.65% Br 37.32% N 6.54% |
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:(II)The treatment of 4-(dimethylamino)benzyl alcohol (I) with concentrated HBr at 120 C in a sealed tube provided benzyl bromide (II). This was then condensed with N-Boc-L-cysteine (III) in the presence of N,N-diisopropyl ethylamine to furnish the benzyl thioether (IV). Subsequent cleavage of the Boc group of (IV) employing HCl in dioxan yielded the intermediate aminoacid (V).
【1】 Miyake, Y.; Horiuchi, M.; Mita, S.; Tsuji, F.; Involvement of leukotriene B4 in murine dermatitis models. Biochem Pharmacol 1998, 55, 297. |
【2】 Kawashima, Y.; Horiuchi, M. (Santen Pharmaceutical Co., Ltd.); Novel amino acid derivs. having N,N-dialkylaminophenyl group. EP 0870762; JP 1996301840; WO 9627585 . |
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) | 41579 | [4-(dimethylamino)phenyl]methanol | 1703-46-4 | C9H13NO | 详情 | 详情 |
(II) | 41580 | 4-(bromomethyl)-N,N-dimethylaniline; N-[4-(bromomethyl)phenyl]-N,N-dimethylamine | C9H12BrN | 详情 | 详情 | |
(III) | 20812 | (2R)-2-[(tert-butoxycarbonyl)amino]-3-sulfanylpropionic acid | 20887-95-0 | C8H15NO4S | 详情 | 详情 |
(IV) | 41581 | (2R)-2-[(tert-butoxycarbonyl)amino]-3-[[4-(dimethylamino)benzyl]sulfanyl]propionic acid | C17H26N2O4S | 详情 | 详情 | |
(V) | 41582 | (2R)-2-amino-3-[[4-(dimethylamino)benzyl]sulfanyl]propionic acid | C12H18N2O2S | 详情 | 详情 |
Extended Information