Biphasic Catalytic Asymmetric Hydrogenation Process

描述（由申请人提供）：药品生产的一个主要变化是当前从批量生产到连续生产的转变。制造成本占行业成本的36%，连续加工可以减少至少90%的运营成本和至少50%的资本支出。FDA和制药行业正在努力将连续加工技术引入制药行业。使用对映选择性催化剂是另一种降低成本的方法。均相催化剂能够产生具有很高对映选择性的手性药物和中间体。不幸的是，这些工艺存在问题，很难从反应混合物中去除昂贵的催化剂，并且制药工业中用于制造活性成分的反应通常以批反应的方式进行。最重要的一类均相手性反应是不对称氢化反应，它被用来制造各种活性成分，包括维生素E、碳青霉烯、S-Oxafloxazin和阿斯巴甜。本提案的目标是开发一种不对称加氢工艺，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 enantioselective 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.