New Biocatalyst for Chiral Synthesis in Organic Media

描述（由申请人提供）：本提案的目标是提高生物催化剂的溶解度、可分离性和可重复使用性，从而增加生物催化在工业化学中的效用。基于在Polium开发实用的、可回收的酶试剂的背景和在TAMU开发用于合成和催化的新型可溶性聚合物支持物的背景，提出了开发可溶性但可回收的聚合物结合的酶试剂的新策略。利用光敏基团和聚丙烯酰胺，我们建议制备脂肪酶生物催化剂，将是可逆的溶解和活性在不同的有机溶剂。下面提出的聚合物载体被设计为提供用于活性酶的载体和回收的手柄，并引入导致有机溶剂溶解性的侧基。此外，这些聚合物-酶缀合物将掺入光敏偶氮芳烃或螺苯并吡喃基团，其在辐照下的几何或结构异构化将改变聚合物的溶解度。结果将是“智能”聚合物结合酶，其在有机溶剂中的溶解度可以通过光照射来打开或关闭。基于洋葱假单胞菌脂肪酶的生物催化剂的靶底物将包括重要的中间体，如β-氨基酸、ACE抑制剂和1-烷氨基-3-芳氧基-2-丙醇的衍生物。所有这些靶标的纯手性形式具有重要的药学应用。 拟议的商业应用：不可用。

DESCRIPTION (provided by applicant): Improvements in biocatalyst solubility, separability and reusability that would increase the utility of biocatalysis in industrial chemistry are the goals of this proposal. Based on a background of development of practical, recoverable enzymatic reagents at Polium and a background in development of novel soluble polymer supports for synthesis and catalysis at TAMU, new strategies to develop soluble but recoverable polymer-bound enzymatic reagents are proposed. Using photoresponsive groups and polyacrylamides, we propose to prepare lipase biocatalysts that will be reversibly soluble and active in different organic solvents. The polymer supports proposed below are designed to provide handles for the support and recovery of active enzymes and to incorporate pendant groups that lead to organic solvent solubility. In addition, these polymer-enzyme conjugates will incorporate photosensitive azoarenes or spirobenzopyran groups whose geometrical or structural isomerization on irradiation will change the polymer's solubility. The result will be 'smart' polymer-bound enzymes whose solubility in organic solvents can be turned on or off by photoirradiation. Target substrates for the biocatalysts based on Pseudomonas cepacia lipase will include important intermediates like beta-amino acids, ACE-inhibitors, and derivatives of 1-alkylamino-3-aryloxy-2-propanol. The homochiral versions of all of these targets have important pharmaceutical applications. PROPOSED COMMERCIAL APPLICATION: Not Available.