Clariant France, Usine de Lamotte, LRA, 60350 Trosly Breuil, France.
Amino Acids. 2012 Aug;43(2):687-96. doi: 10.1007/s00726-011-1117-6. Epub 2011 Oct 21.
The first successful resolution of rac-α-aminoacetals via diastereoisomeric salt formation with optically pure N-protected aminoacids is reported. The absolute configuration assignment of α-aminoacetal enantiomers is performed by an entirely non-racemizing chemical correlation method involving N-protection and a new efficient hydrolysis step followed by a reduction of the resulting N-protected α-aminoaldehyde intermediates. A racemization method of optically enriched α-aminoacetals is exemplified to allow valorisation of both enantiomers.
首次通过与光学纯 N-保护氨基酸形成非对映异构体盐成功拆分了 rac-α-氨基缩醛。通过涉及 N-保护和新的高效水解步骤以及随后还原得到的 N-保护α-氨基醛中间体的完全非消旋化的化学相关方法，实现了对α-氨基缩醛对映异构体的绝对构型分配。光学富集的α-氨基缩醛的外消旋化方法被举例说明，以允许两种对映异构体都得到利用。
