Chiral amidate complexes for the diastereoselective and enantioselective synthesis of chiral amines and N-Heterocycles

催化方法为复杂分子的合成提供了高效节能的途径。胺是组装包括生物碱天然产物、药品和农用化学品在内的广泛目标化合物的关键组成部分。通常所需的胺构建块是手性的，这意味着它们具有不可重叠的镜像（对映体），并且这些对映体在与人类健康治疗中的目标生物受体反应时可以具有不同的性质。因此，对映体胺和含n环化合物（n -杂环）的选择性合成是制药工业日常生产的一个重要方面。实现这些小分子构建块的高效合成的新方法可以减少废物产生并节省制造过程中的成本。Schafer小组最近发现了一个新的催化剂家族，用于从简单胺和烯烃原料中高效合成手性胺，在100%的原子经济反应中（该反应没有副产物）。这种新的反应，即胺的α -烷基化反应，只需要一步就能组装出所需的手性胺产品，没有副产物，通过使用一种合成策略来补充传统的分步路线。勃林格殷格翰加拿大有限公司致力于实现这一新合成转化的全部潜力，并将学术成果扩展到与制药行业相关的小分子领域。此次合作将利用这一新兴技术在制药行业所需胺小分子的竞争性制造中。使用这种催化剂

Catalytic methods afford energy efficient routes for the synthesis of complex molecules. Amines are critical building blocks for the assembly of a broad range of target compounds including alkaloid natural products, pharmaceuticals and agrochemicals. Often the required amine building blocks are chiral, meaning they have non-superimposable mirror images (enantiomers), and these enantiomers can have different properties when reacted with targeted biological receptors in human health treatments. Thus, the selective synthesis of enantiomeric amines and N-containing cyclic compounds (N-heterocycles) is an important aspect of daily production for the pharmaceutical industry. New methods to achieve the efficient syntheses of these small molecule building blocks can result in reduced waste production and cost savings during manufacture. The Schafer group has recently discovered a new family of catalysts for the efficient synthesis of chiral amines from simple amines and alkene feedstocks, in a 100% atom-economic reaction (there are no by-products in this reaction). This new reaction, the alpha-alkylation of amines, assembles the desired chiral amine products in only one step, with no by-products, by using a synthetic strategy that is complementary to traditional step-wise routes. A focused effort to realize the full potential of this new synthetic transformation and to extend academic achievements to small molecules of relevance to the pharmaceutical industry is supported by Boehringer Ingelheim Canada Ltd. This collaboration will exploit this emerging technology in the competitive manufacturing of required amine small molecules for the pharmaceutical industry. Using this catalytic