【结 构 式】 |
【药物名称】Desvenlafaxine Succinate, O-Desmethylvenlafaxine,DVS-233,WY-45233 (as free base) 【化学名称】4-[2-(Dimethylamino)-1-(hydroxycyclohexyl)ethyl]phenol succinate hydrate 【CA登记号】386750-22-7(succinate monohydrate);93413-62-8(free base) 【 分 子 式 】C20H33NO7, 93413-62-8 (as free base, anhydrous) 【 分 子 量 】399.4786 |
【开发单位】Wyeth Pharmaceuticals (US). 【药理作用】Antidepressant, Treatment of postmenopausal syndrome, 5-HT and norepinephrine reuptake inhibitor |
合成路线1
【1】 Gore VG, Kulkarni VS, Patil M. 2009. Process for perparation of O-desmethylvenlafaxine via treatment of venlafaxine with a thiol reagent. WO 2009053731. |
【2】 Modi IA, Muktawat S, Singh UP, et al. 2009. Preparation of O-desmethylvenlafaxine by demethylation of venlafaxine. WO 2009034434. |
【3】 Niddam-Hildesheim V, Nidam T, Dolitzky. 2009. Process for the synthesis of O-desmethylvenlafaxine including tridesmethylvenlafaxime as an intermediate, US 2009069601; US 2008221356. |
【4】 Tyagi OD, Lahari S, Koilkonda P, et al. 2009.Process for producing 1-[2-(dimethylamino)-1-(4-hydroxyphenyl) ethyl] cyclohexanol. WO 20090840039. |
【5】 Srinivasan CV, Aggarwal AK, Sarin GS, et al. 2009. Improved process for the preparation of O-desmethyl-venlafaxine. WO 2009084038. |
【6】 Xu JK, Xu MD, Cai YX, et al.2009.Novel method for preparation of O-desvenlafaxine. 发明专利申请公开说明书. CN 101117320. |
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) | 32753 | 2-(4-hydroxyphenyl)acetonitrile; 4-Hydroxybenzyl cyanide | 14191-95-8 | C8H7NO | 详情 | 详情 |
(II) | 67072 | 2-(4-(benzyloxy)phenyl)acetonitrile 英文名称为: | C15H13NO | 详情 | 详情 | |
(III) | 11059 | Cyclohexanone | 108-94-1 | C6H10O | 详情 | 详情 |
(IV) | 67073 | 2-(4-(benzyloxy)phenyl)-2-(1-hydroxycyclohexyl)acetonitrile | C21H23NO2 | 详情 | 详情 | |
(V) | 67074 | 1-(2-amino-1-(4-(benzyloxy)phenyl)ethyl)cyclohexanol | C21H27NO2 | 详情 | 详情 |
合成路线2
【1】 Gore VG, Kulkarni VS, Wakchaure VS, et al. 2008. Process for perparation of O-desmethyl venlafaxine(ODV) from phenylacetic acid derivatives, dimethylamino, and cyclohexanone. WO 2008093142. |
【2】 Niddam-Hildesheim V, Shenkar N, Shachan-Tov S. 2008. Process for the synthesis of O-desmethylvenlafaxine from 1-[2-amino-1-(4-methoxyphenyl) ethyl] cyclohexanol via O-demethylation and N-methylation reactions. WO 2008013995. |
【3】 Niddam-Hildesheim V, Shenkar N, Shachan-Tov S. 2008. Process for the synthesis of O-desmethylvenlafaxine from hydroxybenzyl cyanide via condensation reaction with cyclohexanone. WO 2008013993. |
【4】 Niddam-Hildesheim V, Shenkar N, Shachan-Tov S. 2008. Process for the synthesis of O-desmethylvenlafaxine from (4-hydroxyphenyl) acetic acid. WO 2008013990. |
【5】 Zupancic S, Skrabanja V. 2007. Process for praparation of O-desmethylvenlafaxine. WO 2007147564. |
中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
---|---|---|---|---|---|---|
(II) | 67076 | 2-(4-(benzyloxy)phenyl)acetyl chloride | C15H14ClO2 | 详情 | 详情 | |
(I) | 67075 | 2-(4-(benzyloxy)phenyl)acetic acid | C15H14O3 | 详情 | 详情 | |
(III) | 67077 | 2-(4-(benzyloxy)phenyl)-N,N-dimethylacetamide | C17H20NO2 | 详情 | 详情 | |
(IV) | 11059 | Cyclohexanone | 108-94-1 | C6H10O | 详情 | 详情 |
(V) | 67078 | 2-(4-(benzyloxy)phenyl)-2-(1-hydroxycyclohexyl)-N,N-dimethylacetamide | C23H30NO3 | 详情 | 详情 |
Extended Information