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Here, we report a three-component coupling reaction approach between an aldehyde, an allyloxyamine, and a maleimide toward isoquinoline derivatives. At first, an oxime O-allylic ether, prepared by dehydrative condensation of the aldehyde and the allyloxyamine, was reacted with the maleimide in the presence of a Pd 2+ species. The cycloadduct obtained was then subjected to the Heck cyclization...
Here, we report a diversity-oriented synthetic approach toward skeletally diverse, cyclized peptidomimetics with diverse appendages. Starting from α-(N-acylamino)amides with various appendages, 12 to 16-membered lactams with defined olefin geometry were synthesized by a common synthetic sequence. We also synthesized the macrocycle in a liquid phase directed toward a construction of the peptidomimetics...