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We report herein the use of the multi-component boronic Mannich reaction (BMR) in a solid-phase approach, in which an aryl boronic acid is combined with an aldehyde and a secondary amine. We describe several examples, in which each of the three components is alternately anchored onto Wang polystyrene, giving in most cases (but not all) the expected products in high yields and purities. We also suggest,...
The focus of this paper is the chemistry of 2-piperazinones and the use of this building block to restrict the conformational freedom of the growth secretagogue NN703 (currently in clinical development). We exploit classical methods for 2-piperazinone synthesis as well as some novel approaches such as a Boronic Mannich reaction. Finally, we report on the ability of the constrained target compounds...
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