Biphasic Catalytic Asymmetric Hydrogenation Process

描述（由申请方提供）：药品生产的一个主要变化是目前从批量生产转变为连续生产。制造成本占行业成本的36%，连续加工可以减少至少90%的运营费用和至少50%的资本费用。FDA和制药业正在努力将连续加工引入制药业。使用对映选择性催化剂是降低成本的另一种手段。均相催化剂能够以非常高的对映选择性制备手性药物和中间体。不幸的是，这些方法存在问题，从反应混合物中除去昂贵的催化剂非常困难，并且在制药工业中用于制备活性成分的反应通常以间歇反应进行。最重要的一类均相手性反应是不对称氢化，其用于制备各种活性成分，包括维生素E、碳青霉烯、S-氧氟沙星和阿斯巴甜。该提案的目标是开发一种不对称氢化方法，该方法允许手性催化剂的连续进料、反应、分离和再利用，从而显著节省工艺成本。

DESCRIPTION (provided by applicant): A major change in pharmaceutical manufacturing is the current shift from batch to continuous processing. Manufacturing costs account for 36% of the industries costs and continuous processing can reduce operating expenses by at least 90% and capital expenses by at least 50%. The FDA and industry are working to bring continuous processing to pharmaceutical manufacturing. The use of enantioselectivity catalysts is another means to reduce costs. Homogeneous catalysts are able to produce chiral drugs and intermediates with very high enantioselectivity. Unfortunately, these processes suffer problems, it is very difficult to remove the expensive catalyst from the reaction mixture and the reactions used to make active ingredients in the pharmaceutical industry have typically been carried out as batch reactions. One of the most important classes of homogeneous chiral reactions is asymmetric hydrogenation, which is used to make a variety of active ingredients, including Vitamin E, Carbapenem, S-Oxafloxazin and Aspartame. The goal of this proposal is to develop an asymmetric hydrogenation process that allows the continual feed, reaction, separation and reuse of a chiral catalyst resulting in dramatic saving in process costs.