铑(III)催化的化学反应引起了有机化学界的广泛关注，尤其是环状的铑杂物种，具有良好的环化反应活性。本项目拟发展铑(III)催化的杂环化合物的合成方法学及其在药物合成中的应用研究：(1)利用简单易得的苯磺酰胺类化合物，在铑(III)催化剂作用下形成的环状铑物种，与各类炔烃、烯烃、烯烃环丙烷、重氮、CO等进行环化反应，简洁高效地合成各类苯磺酰胺杂环化合物；(2)对吲哚、吡咯类化合物进行简单的衍生化，构建氧化性酰胺导向基团，在铑(III)催化剂作用下形成的环状铑物种，与各类炔烃、烯烃、重氮、CO、苯硼酸等进行环化反应，简洁高效地构建各类吲哚并环、吡咯并环化合物，并且应用于若干中枢神经系统药物的新合成；(3)以含有手性辅助基团的重氮化合物为原料，在铑(III)催化剂作用下，与各类苯甲酰胺、苯磺酰胺、N-吲哚酰胺类化合物进行环化反应，对新形成的季碳诱导手性，合成各类光学纯的杂环类化合物。

Recently, the chemistry of Rh(III)-catalysis has received significant attention in organic synthesis. In particular, the Rh(III)-derived rhodacycles show high efficiency in cyclization. In the course of our research on metal-catalyzed cyclization for access to heterocycle, we envisioned that benzene sulfonamides containing oxidative directing group, could enable rhodacycles formation in the presence of Rh(III) catalysis, and late-stage redox-neutral cyclization with various alkynes, alkenes, methylenecyclopropanes, diazo compounds and CO, to construct diverse heterocycles in high efficiency under mild condition. Also, the indoles and pyrroles could be simply derived to N-carboxamides with oxidative directing group, and their cyclization with alkynes, alkenes, diazo compounds，CO and aryl boronic acids under Rh(III) catalysis could lead to rapid construction of various indole-fused and pyrrole-fused heterocycles; furthermore, this protocol could be applied to concise synthesis of central nervous system (CNS) drugs. Another proposal is that the use of chiral auxiliary containing diazo compounds in Rh(III)-catalyzed cyclization with benzamides, benzene sulfonamides and N-carboxamide of indoles, could undergo asymmetric induction in stereogenic center formation, thus leading to synthesis of heterocycles in high enantioselectivity.