由sRuPhos启用的Atroposelective Suzuki-Miyaura合形成2-Amino-2'-Hydroxybiphenyls,使其成为可能
Hamzah Sharif1, Luke A McCall1, Matthew G Sanders2
1Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK.
一种新的性素连接体,sRuPhos,使得高效的不对称的Suzuki-Miyaura合能够产生有价值的atropisomeric biaryls. 这种方法在没有浪费分离的情况下实现了用于制药应用的高反选择性.
科学领域:
- 有机化学 有机化学
- 不对称的催化剂.
- 药用化学 医学化学
背景情况:
- 在制药中,亚特罗皮索默性比亚尔基是至关重要的.
- 不对称的木-米亚乌拉合是这些化合物的直接途径.
- 以前的方法需要浪费的分离或分辨率.
研究的目的:
- 开发一种用于不对称的苏苏基-米亚乌拉合的新型合性氨酸接体.
- 为了合成具有高反选择性的2-amino-2'-hydroxybiphenyls.
- 为了探索配体对具有挑战性的基质的实用性.
主要方法:
- 使用了一种新的硫化素连接体,sRuPhos.
- 采用了不对称的苏苏基-米亚乌拉合反应.
- 结合未受保护的正甲和正甲酸.
主要成果:
- 实现了高达99%的极高反体过剩 (ee).
- 成功合成了2-氨基-2'-基双.
- 证明了N-化和形成高度阻碍的双的适应.
结论:
- sRuPhos 是一种有效的配体,用于合成有价值的亚特罗皮索米二甲基.
- 开发的方法为复杂的二基结构提供了一条有效的途径.
- sRuPhos在不对称的催化反应中显示出更广泛应用的潜力.
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