3-（2,5-二氢-1H-吡咯-2-基甲氧基）吡啶：合成与镇痛活性
3-(2,5-Dihydro-1H-pyrrol-2-ylmethoxy)pyridines: synthesis and analgesic activity.
作者信息
Baraznenok Ivan L, Jonsson Emma, Claesson Alf
机构信息
Syntagon AB, Tallvägen 2, Box 2073, SE-15102 Södertälje, Sweden.
出版信息
Bioorg Med Chem Lett. 2005 Mar 15;15(6):1637-40. doi: 10.1016/j.bmcl.2005.01.058.
PMID:15745813
Abstract
We disclose an efficient procedure for the preparation of ethers of 2-substituted 2-hydroxymethylpyrroline and of 2-aminomethyl-3-pyrrolines, involving, as a key step, formation and nucleophilic ring opening of a cyclic sulfamidate. Several new analogs of epibatidine (1) and tebanicline (ABT-594, 2) were prepared and tested for analgesic activity in the mouse formalin model.
摘要
我们公开了一种制备2-取代-2-羟甲基吡咯啉醚和2-氨甲基-3-吡咯啉醚的有效方法，该方法的关键步骤是环状氨基磺酸酯的形成和亲核开环。制备了几种埃博霉素（1）和替巴尼林（ABT-594，2）的新类似物，并在小鼠福尔马林模型中测试了它们的镇痛活性。
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