Department of Applied Chemistry, China Agricultural University , Beijing 100193, P. R. China.
Institute of High Energy Physics, Chinese Academy of Science , Beijing 100049, P. R. China.
Org Lett. 2016 Nov 4;18(21):5644-5647. doi: 10.1021/acs.orglett.6b02885. Epub 2016 Oct 21.
With the use of a commercially available chiral phosphine as the catalyst, the first catalytic enantioselective [4 + 3] annulation of allenoates with C,N-cyclic azomethine imines is developed. The reaction works efficiently under mild reaction conditions to afford seven-membered ring-fused quinazoline-based tricyclic heterocycles in high yields with good to excellent diastereo- and enantioselectivities.
在手性膦配体的催化下,首次实现了丙二酸盐与 C,N-环亚胺基烯酮的[4+3]环加成反应,该反应条件温和,以高产率、优异的非对映选择性和对映选择性得到了七元环稠合的基于喹唑啉的三环杂环化合物。