パラジウム触媒を用いた分子内シアノアミド化反応の開発とベンゾアゼピンアルカロイド合成への展開

抄録

Palladium-catalyzed intramolecular cyanoamidation of 1,1-disubstituted alkenyl cyanoformamides proceed in 68-100% yield to afford oxindoles bearing a quaternary carbon center, which are key intermediates for the synthesis of alkaloids such as physostigmine. Practically, esermethol was synthesized via the reductive cyclization of the product in 22% yield in 6 steps. The reaction was also applied to alkynyl cyanoformamides to give the five- to seven-membered lactams having tetrasubstituted alkenes in high yield. The application of the products to the synthesis of benzoazepine alkaloids are under investigation.

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