【结 构 式】 |
【分子编号】63528 【品名】3-({8-[2-(acetylamino)ethyl]-2-naphthalenyl}oxy)propyl methanesulfonate 【CA登记号】 |
【 分 子 式 】C18H23NO5S 【 分 子 量 】365.45036 【元素组成】C 59.16% H 6.34% N 3.83% O 21.89% S 8.77% |
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:(V)Demethylation of N-[2-(7-methoxynaphth-1-yl)ethyl]acetamide (I) with boron tribromide-dimethyl sulfide complex affords phenol (II). This is then alkylated with 3-bromopropanol (III) in the presence of K2CO3 to provide the hydroxypropyl derivative (IV). After conversion of alcohol (IV) into the corresponding mesylate (V), condensation with a further equivalent of phenol (II) in hot DMF furnishes the target dimeric compound
【1】 Guillaumet, G.; Renard, P.; Lesieur, D.; Yous, S.; Descamps-Francois, C.; Lefoulon, F.; Viaud, M.-C.; Delagrange, P.; Bennejean, C. (ADIR et Cie.); Substd. dimeric cpds., process for their preparation and pharmaceutical compsns. thereof. EP 1038863; FR 2791344; JP 2000319242; US 2002035114; US 6319930; US 6635650 . |
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) | 63525 | N-{2-[7-(methyloxy)-1-naphthalenyl]ethyl}acetamide | C15H17NO2 | 详情 | 详情 | |
(II) | 63526 | N-[2-(7-hydroxy-1-naphthalenyl)ethyl]acetamide | C14H15NO2 | 详情 | 详情 | |
(III) | 12573 | 3-Bromo-1-propanol; 3-Bromopropanol | 627-18-9 | C3H7BrO | 详情 | 详情 |
(IV) | 63527 | N-(2-{7-[(3-hydroxypropyl)oxy]-1-naphthalenyl}ethyl)acetamide | C17H21NO3 | 详情 | 详情 | |
(V) | 63528 | 3-({8-[2-(acetylamino)ethyl]-2-naphthalenyl}oxy)propyl methanesulfonate | C18H23NO5S | 详情 | 详情 |
Extended Information