Rönnholm Petra, Södergren Mikael, Hilmersson Göran
Department of Chemistry, Göteborg University, Kemivägen 10, SE-412 96 Göteborg, Sweden.
Org Lett. 2007 Sep 13;9(19):3781-3. doi: 10.1021/ol701504c. Epub 2007 Aug 16.
A robust and scaleable route to chiral 1-isopropylamino-2-(diphenylphosphino)ethanes is described via the ring-opening of chiral, cyclic sulfamidates with potassium diphenylphosphide (KPPh(2)). The novel protocol offers a robust access to gram quantities of chiral amino phosphinoethanes in high yields. The Li-amides of the chiral aminophosphines were evaluated as chiral ligands in the asymmetric addition of n-butyllithium (BuLi) to benzaldehyde, yielding 1-phenylpentanol up to 98% ee.
本文描述了一种通过手性环状氨基磺酸酯与二苯基膦钾（KPPh₂）开环反应制备手性1-异丙基氨基-2-（二苯基膦基）乙烷的稳健且可扩展的方法。该新方法能够以高产率稳健地制备克级量的手性氨基膦基乙烷。对手性氨基膦的锂酰胺在正丁基锂（BuLi）不对称加成到苯甲醛反应中作为手性配体进行了评估，得到对映体过量（ee）高达98%的1-苯基戊醇。
