催化酶选择性乳和乳的联合还原
Gregory Hughes1, Masanari Kimura, Stephen L Buchwald
1Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA.
Journal of the American Chemical Society
|October 14, 2005
概括
酒精添加剂极大地加快了对抗选择性铜催化合降解反应. 这种高效的方法,使用易于获得的材料,实现了各种不和化合物的高产量和酶选择性.
科学领域:
- 有机化学 有机化学
- 催化剂是一种催化剂.
- 不对称的合成方法
背景情况:
- 结合物还原是有机合成中的一个关键转换.
- 选择性方法对于产生性分子至关重要.
- 铜催化提供了一种具有成本效益和多功能性的方法.
研究的目的:
- 开发一种高度加快和选性铜催化合物减少方法.
- 研究酒精添加剂对反应效率的影响.
- 为了证明开发的方法在合成有价值的制药中间体中的适用性.
主要方法:
- 在现场生成催化剂使用铜二酸盐 (CuCl2) H2O),三氧化物 (t-BuONa) 和p-tol-BINAP.
- 使用聚甲基西洛 (PMHS) 作为减少剂.
- 添加酒精添加剂以加快反应速度.
主要成果:
- 显著加快对α,β不和乳,乳和的酶选择性结合降解.
- 在一系列基板上实现良好的至优秀的产量和酶选择性.
- 成功地将该方法应用于合成 (-) -Paroxetine,这是一个关键的药物化合物.
结论:
- 酒精添加剂显著提高了铜催化酶选择性结合物减少的速度.
- 开发的方法提供了一个高效和实用的途径,以奇拉不和化合物.
- 这种方法对包括药品在内的复杂分子的可扩展合成具有前景.
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