Catalytic Enantioselective Strain Release For The Synthesis Of Chiral Cycloalkanes

由于全球人口不断增加，预计2050年粮食生产需求将增加70%。因此，粮食安全在世界范围内具有重要意义。在这方面，拟除虫菊酯类杀虫剂在减少害虫造成的产量损失和提高农业生产率方面发挥着重要作用。在这次会议期间，我们建议利用我们的模块化和可调的超碱催化平台，设计、发现和开发新的亚胺基膦催化体系，使手性亚胺基环丙烷(ACPs)的对映选择性合成成为可能，从而实现手性环丙烷库的高效合成。鉴于环丙烷在天然产物和药物分子中的广泛应用，如上市的抗血小板药物替卡格雷和抗病毒药物环丙韦，该策略可以进一步应用于拟除虫菊酯类杀虫剂和生物相关产品的对映选择性合成。同样，这一策略也适用于构建富含对映体的环丁烷，这些环丁烷也是生物活性分子中的常见基序，也是有机合成中的多种中间体。这项建议既包括向东道国机构转让知识，也包括对候选人进行新的先进技术培训。研究结果具有在工业生产中应用的潜力(即拜耳)。

Demand for food production is projected to increase by 70% in 2050 due to increasing global population. As such, food security is of vital significance worldwide. In this regard, pyrethroid insecticides, which usually feature gem-dimethyl cyclopropane core, play an important role in reducing the yield losses caused by pests and increase the productivity of agriculture.During this Fellowship, we propose to exploit our modular and tunable superbase catalyst platform, to design, discover and develop new iminophosphorane catalyst systems that will allow the enantioselective synthesis of chiral alkylidenecyclopropanes (ACPs), thus achieving the efficient synthesis of a library of chiral cyclopropanes. Given that cyclopropanes' prevalence in natural products and pharmaceutical molecules like marketed antiplatelet drug Ticagrelor and antiviral cyclopropavir, this strategy can be further applied in the enantioselective synthesis of pyrothroid insecticides and biologically relevant products. In a similar vein, this strategy would be applicable in the construction of enantioenriched cyclobutanes, which are also common motifs in bioactive molecules and versatile intermediates in organic synthesis. This proposal includes both the transfer of knowledge to the host institution and the training of the candidate in new advanced techniques. Results have the potential capacity to be applied in industrial production (i.e. Bayer).