CVMED Chemistry, Pfizer Worldwide Research and Development, 445 Eastern Point Road, Groton, Connecticut 06340, USA.
Org Lett. 2013 Jul 5;15(13):3424-7. doi: 10.1021/ol401477r. Epub 2013 Jun 21.
Achiral [3.2.1] bridged heterocycles containing a bridging amide can undergo enantioselective hydroarylation reactions under rhodium(I) catalysis. These reactions proceed in high yield and enantioselectivity in most cases, under mild reaction conditions and using commercially available Josiphos ligands. The phosphine ligand structure and the protecting group on the nitrogen both have significant effects on the selectivity and yield of the reactions.
手性[3.2.1]桥连杂环含有桥连酰胺，在手性铑（I）催化下可以进行对映选择性的氢芳基化反应。在温和的反应条件下，使用商业可得的 Josiphos 配体，这些反应在大多数情况下以高产率和对映选择性进行。膦配体结构和氮上的保护基对反应的选择性和产率都有显著影响。
