转氨酶触发的2,5-非替代型罗利丁的合成
Aoife Martin1, Lisa Kennedy1, Ishita Solanki1
1School of Chemistry, University College Dublin, Belfield, Dublin 4, Ireland. elaine.oreilly@ucd.ie.
研究人员通过转氨酶催化的分子内阿扎-迈克尔反应从基因中合成了2,5-非替代型罗利丁. 一种新的表皮化方法选择性地产生了cis-pyrrolidines,增强了有机合成中的 diastereoselectivity.
科学领域:
- 有机化学 有机化学
- 合成化学 合成化学
- 药用化学 医学化学
背景情况:
- 罗利丁是药品中至关重要的异环化合物.
- 对立体定义的罗利丁的高效合成仍然是一个挑战.
研究的目的:
- 开发一种新型合成途径,以获得2,5-非替代型罗利丁.
- 建立一种方法来控制pyrrolidine合成中的 diastereoselectivity.
主要方法:
- 转胺酶催化基因的分子内阿扎-迈克尔反应.
- 开发一种新型的表皮化协议.
主要成果:
- 获得了2,5-非替代型罗利丁的中等到良好的产量.
- 一种新型的表皮化策略成功地分离了具有高二选择性的cis-N-nosyl-protected pyrrolidines.
- 该方法对大多数衍生品有效,不包括.
结论:
- 转胺酶触发的阿扎-迈克尔反应提供了进入罗利丁支架的途径.
- 开发的表皮化提供了一条通往二聚体纯的cis-pyrrolidines的途径.
- 这种方法对于构建含有罗利丁的复杂分子非常有价值.
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