公开(公告)号：US20090018343A1

公开(公告)日：2009-01-15

申请号：US11886417

申请日：2006-03-16

申请人： Philip Gregory Hultin ,  Jason Ellis Hein

发明人： Philip Gregory Hultin ,  Jason Ellis Hein

IPC分类号： C07D263/22

CPC分类号： C07D263/22

摘要： The present invention relates generally to perfluoroalkyl chiral auxiliary compounds and methods of manufacture. These compounds have the functionality to effectively support the synthesis of chiral compounds in single reactions, high-throughput parallel reactions, or combinatorial reactions The invention relates to two oxazolidinone chiral auxiliaries (1) and (2): wherein Rf is a perfluoroalkyl group having the general formula (CH2)x—CyF2y+1 where x=1-5 and y=4-10 and wherein B is an unfunctionalized aryl, alkyl or arylalkyl group in a preferred embodiment, x=2 and y=6 and B is derived from unfunctionalized amino acids The amino acids may be from either the D- or L-series, and are preferably enantiomerically pure or in very high enantiomeric excess in either configuration.

摘要翻译： 本发明一般涉及全氟烷基手性助剂及其制备方法。 这些化合物具有有效支持单反应，高通量平行反应或组合反应中手性化合物合成的功能。本发明涉及两种恶唑烷酮手性助剂（1）和（2）：其中Rf是具有 通式（CH2）x-CyF2y + 1其中x = 1-5和y = 4-10，其中B是优选实施方案中未官能化的芳基，烷基或芳烷基，x = 2和y = 6，B衍生 来自未官能化的氨基酸氨基酸可以来自D-或L-系列，并且优选对映异构体纯或在任何构型中具有非常高的对映体过量。