在连续流中进行酶选择性合成:聚合物支持的异尿酶催化酶选择性迈克尔添加-循环化与α-Azol-2-ylacetophenones
Zhanyu Zhou1, Kevin Kasten1, Tengfei Kang1
1EaStCHEM, School of Chemistry, University of St. Andrews, North Haugh, St. Andrews KY16 9ST, U.K.
概括
这项研究引入了一种连续流程方法,用于使用聚合物支持的催化剂合成奇拉性异环化合物. 该工艺实现了高产量和优异的纯度,证明了实际应用的可扩展性.
科学领域:
- 有机化学 有机化学
- 催化剂是一种催化剂.
- 流动化学 流动化学
背景情况:
- 对药品而言,对异环化合物的酶选择性合成至关重要.
- 开发高效,可扩展的催化系统仍然是一个挑战.
研究的目的:
- 开发一个连续流程的过程,以对异环环的enantioselective合成.
- 为了利用聚合物支持的同位素尿素催化剂 (HyperBTM) 进行这种转化.
主要方法:
- 使用一个装满了聚合物支持的异尿素HyperBTM催化剂的反应堆床.
- 使用了α-azol-2-ylacetophenones和-acetamides与α,β-不和同类化物在连续流中.
- 研究了α,β-不和酸中间体的形成.
主要成果:
- 实现了各种异环制品的合成,以良好的到优秀的产量.
- 获得的产品具有优异的纯度,最高可达97:3 er.
- 证明成功扩展到15毫摩尔尺度,总体产量为68%,再结晶后为98: 2 时.
结论:
- 开发的连续流程方法是有效的 enantioselective 异环合成.
- 聚合物支持的HyperBTM催化剂能够高效且可扩展地生产性异环.
- 这种方法提供了一条有前途的途径,用于获取基纯异环化合物.
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