Organic Synthesis Reagents on Transition Metals

描述(由申请人提供)：复杂分子中碳-碳键的合成对于构建新的药物制剂是必不可少的。在过去的几年里，烯烃复分解反应已经成为合成此类化合物的一种新的通用方法。这一转变的关键是活性、高效和选择性的催化剂的可用性。在过去的几年里，已经开发了一系列催化剂，这些催化剂在大量未保护的官能团存在的情况下表现出高活性。进一步的应用将需要对映体和立体选择性的催化剂，并将在高度官能化的烯烃上进行歧化反应。在上一个授权期内，在开发指导配体设计的模型方面取得了进展。在接下来的授权期内，该模型将被用于构建新的配体体系，用于立体选择性交叉复分解反应(控制形成的双键的E：Z比)，并提高空间受阻的烯烃的反应活性。各种新的N-杂环卡宾配体将被制备出来，这些配体不仅在制备选择性烯烃歧化催化剂方面具有应用价值，而且在催化剂设计中也具有普遍的用途。这种催化剂的成功构建将为构建生物活性分子开辟有效的新途径。

DESCRIPTION (provided by applicant): The synthesis of carbon-carbon bonds in complex molecules is essential for the construction of new pharmaceutical agents. Over the past several years, olefin metathesis has become a new general method for the construction of such compounds. Key to this transformation is the availability of catalysts that are active, efficient and selective. Over the past several years, a family of catalysts has been developed that shows high activity in the presence of a wide array of unprotected functional groups. Further applications will require catalysts that are enantio and stereoselective and will carry out metathesis on highly functionalized olefins. During the last granting period, progress was made in the development of a model to direct ligand design. During the next granting period, this model will be used to construct new ligand systems for enantioselective cross metathesis, for the stereoselective (control the E:Z ratio of the double bonds formed) in cross metathesis and increase the reactivity of sterically hindered olefins. A variety of new N-heterocyclic carbene ligands will be prepared that will not only have applications in the preparation of selective olefin metathesis catalysts but will be of general use in catalyst design. Successful construction of such catalysts will open efficient new routes to the construction of bioactive molecules.