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【结 构 式】 
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【分子编号】13606 【品名】1-(Dimethylamino)-3-[2-(3-methoxyphenethyl)phenoxy]-2-propanol 【CA登记号】 |
【 分 子 式 】C20H27NO3 【 分 子 量 】329.43932 【元素组成】C 72.92% H 8.26% N 4.25% O 14.57% |
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：(IV)The reaction of 2-hydroxy-3'-methoxybibenzyl (I) with epichlorohydrin (II) by means of NaH in DMF gives 2-(2,3-epoxypropoxy)-3'-methoxybibenzyl (III), which by reaction with dimethylamine in refluxing THF yields 2-[3-(dimethylamino)-2-hydroxypropoxy]-3'-methoxybibenzyl (IV). Finally, this compound is treated with succinic anhydride (V) in refluxing THF and with HCl in acetone.
| 【1】 Kikumoto, R.; Fukami, H.; Hara, H.; Ninomiya, K.; Sugano, M. (Mitsubishi Chemical Corp.); Pharmaceutically active (3-aminopropoxy)-bibenzyl derivs. EP 0072942 . |
| 【2】 Prous, J.; Castaner, J.; Sarpogrelate Hydrochloride. Drugs Fut 1992, 17, 12, 1093. |
| 【3】 Osakabe, M.; Fukami, H.; Sugano, M.; Kikumoto, R.; Ninomiya, K.; Tamao, Y.; Hara, H.; Syntheses and platelet aggregation inhibitory and antithrombotic properties of [2-[(omega-aminoalkoxy)phenyl]ethyl]benzenes. J Med Chem 1990, 33, 6, 1818. |
| 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) | 10146 | Epichlorohydrin; 2-(Chloromethyl)oxirane | 106-89-8 | C3H5ClO | 详情 | 详情 |
| (II) | 13604 | 2-(3-Methoxyphenethyl)phenol | C15H16O2 | 详情 | 详情 | |
| (III) | 13605 | 2-(3-Methoxyphenethyl)phenyl 2-oxiranylmethyl ether; 2-[[2-(3-Methoxyphenethyl)phenoxy]methyl]oxirane | C18H20O3 | 详情 | 详情 | |
| (IV) | 13606 | 1-(Dimethylamino)-3-[2-(3-methoxyphenethyl)phenoxy]-2-propanol | C20H27NO3 | 详情 | 详情 | |
| (V) | 11291 | Dihydro-2,5-furandione; Succinic anhydride | 108-30-5 | C4H4O3 | 详情 | 详情 |
Extended Information