ENANTIOSELECTIVE SYNTHESIS OF AMINO ACIDS

氨基酸是蛋白质的主要成分， 生物体重要的基本营养素。 他们也是 有价值的合成中间体，用于制备大量 一系列生物活性化合物， 医药行业。 基于氨基酸的药物实例 左旋多巴，色氨酸和β-内酰胺类抗生素 不幸的是，典型的氨基酸生产方法需要 获得昂贵且耗时的光学分辨率 光学纯产品 制备氨基酸的更理想的方法是 对映选择性碳-氮双键 （C=N）氨基酸前体基团。 这种直接合成 因为只生成所需的产品， 避免了手性分离的费用。 可惜 目前的催化剂通常没有足够的活性或选择性 足以在工业上使用。 本提案的目的是 通过对映选择性制备光学纯氨基酸， 具有C=N键的化合物的氢化，并显示 各种氨基酸可以经济地生产， 工业规模。 建议的商业应用 本研究将为开发通用的 通过对映体选择性制备光学纯氨基酸 具有C=N键的化合物的氢化。 这将允许 经济地生产有价值的氨基酸， 医药和合成中间体。

Amino acid are the main components of proteins and are important elementary nutrients for living organisms. They are also valuable synthetic intermediates for the preparation of a large array of biologically active compounds important to the pharmaceutical industry. Examples of drugs based on amino acids are L-DOPA, L-tryptophan, and beta-lactam antibiotics. Unfortunately, typical production methods for amino acids require expensive and time-consuming optical resolutions to obtain optically pure products. A more desirable way to prepare amino acids would be to enantioselectively hydrogenate carbon-nitrogen double bond (C=N) groups of amino acid precursors. This direct synthesis route could lower costs because only the desired product is formed avoiding the expense of a chiral separation. Unfortunately, the current catalysts generally are not sufficiently active or selective enough to be industrially useful. The objective of this proposal is to prepare optically pure amino acids by enantioselective hydrogenation of compounds with C=N bonds and to show that a variety of amino acids can be economically produced on an industrial scale. PROPOSED COMMMERCIAL APPLICATION This research will lead to the development general method for the production of optically pure amino acids by the enantioselective hydrogenation of compounds with C=N bonds. This will allow the economical production of valuable amino acids for use as pharmaceuticals and synthetic intermediates.