Catalytic Enantioselective Strain Release For The Synthesis Of Chiral Cycloalkanes

由于全球人口不断增加，预计到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至关重要的意义。因此，以宝石-二甲基环丙烷为核心的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力方面发挥了重要作用。在本次合作中，我们将利用我们的模块化和可调超碱催化剂平台，设计、发现和开发新的亚磷磷烷催化剂体系，以实现手性烷基环丙烷（ACPs）的对手性选择性合成，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普遍存在，如已上市的抗血小板药物替格瑞洛和抗病毒药物环丙帕韦，该策略可以进一步应用于菊酯类杀虫剂和生物相关产品的对构象选择性合成。同样，这种策略也适用于构建富含对映体的环丁烷，这也是生物活性分子和有机合成中多功能中间体的常见基序。这一建议既包括向东道国机构转移知识，也包括对候选人进行新的先进技术培训。结果具有应用于工业生产（即拜耳）的潜在能力。

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).