Graduate School of Pharmaceutical Sciences, Kyoto University , Sakyo-ku, Kyoto 606-8501, Japan.
Org Lett. 2017 Jul 21;19(14):3875-3878. doi: 10.1021/acs.orglett.7b01759. Epub 2017 Jul 10.
A gold-catalyzed cascade reaction of skipped diynes (1,4-diynes) and pyrroles has been developed. This reaction proceeds by the consecutive regioselective hydroarylation of two alkynes with a pyrrole, followed by a 7-endo-dig cyclization to give 1,6-dihydrocyclohepta[b]pyrroles in good yields. The direct synthesis of cyclohepta[b]indoles using indole nucleophiles has also been reported.
发展了一种金催化的缺二炔(1,4-二炔)和吡咯的级联反应。该反应通过与吡咯的两个炔烃的连续区域选择性氢芳基化反应,然后进行 7-endo-dig 环化反应,以良好的收率得到 1,6-二氢环庚[b]吡咯。还报道了使用吲哚亲核试剂的直接合成环庚[b]吲哚。