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【结 构 式】 
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【分子编号】16127 【品名】3-Hydroxyquinuclidine borane complex 【CA登记号】 |
【 分 子 式 】C7H16BNO 【 分 子 量 】141.02118 【元素组成】C 59.62% H 11.44% B 7.67% N 9.93% O 11.35% |
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：(I)The condensation of 3-hydroxy-1-azabicyclo[2.2.2]octan borane complex (I) with 2-propynyl bromide (II) by means of NaH in DMF gives racemic 3-(2-propynyloxy)-1-azabicyclo[2.2.2]octane (III), which is then submitted to optical resolution with (+)- or (-)-dibenzoyltartaric acid. The optically pure tartrates are treated with aqueous K2CO3 and finally with fumaric acid to obtain the optically pure fumarates.
| 【1】 Walther, G.; Weber, K.-H.; Stransky, W.; Kuhn, F.; Müller, E.; Ensinger, H. (Boehringer Ingelheim GmbH); Novel quinuclidines, their pharmaceutical use and process for their preparation. AU 8945403; DE 3839385; EP 0370415; JP 1990243688; US 5286864; US 5451587 . |
| 【2】 Mealy, N.; Prous, J.; Castaner, J.; WAL-2014-FU. Drugs Fut 1994, 19, 1, 35. |
Extended Information