Nickel-Catalyzed Synthesis and N-Arylation of Biologically Active Sulfonamides

大多数药物化合物的有益性质来自于含氮官能团的存在，包括磺酰胺结构基元。这一合作研究项目将寻求利用申请人的研究小组在可持续催化方面开发的最新专业知识，以解决工业合作伙伴(蒙特利尔ParazaPharma Inc.，QC)在专有活性药物成分中有针对性地合成和/或修改生物活性磺胺化合物方面面临的具体未解决的挑战。特别是，工业伙伴需要温和的路线来获得生物活性的磺胺类化合物，以及这些化合物的N-官能化，理想地利用廉价和丰富的试剂(例如，胺、(杂)芳基氯化物)，并利用地球丰富的催化剂(而不是贵金属催化剂)。一旦开发出来，ParazaPharma公司的科学家可以直接利用这些合成协议进行专利原料药合成/药物开发。该项目的成功将大大加快工业合作伙伴的药物开发计划，从而更快地确定新的治疗方法，使所有加拿大人受益。

The majority of pharmaceutical compounds derive their beneficial properties from the presence of nitrogen-containing functional groups, including the sulfonamide structural motif. This collaborative research project will seek to exploit recent expertise in sustainable catalysis developed by the applicant's research group, in addressing specific unmet challenges faced by the industrial partner (ParazaPharma Inc., Montreal, QC) with regard to the targeted synthesis and/or modification of biologically active sulfonamide compounds within proprietary active pharmaceutical ingredients. In particular, the industrial partner requires mild routes to biologically active sulfonamides, as well as the N-functionalization of such compounds, ideally exploiting cheap and abundant reagents (e.g., amines, (hetero)aryl chlorides), and making use of Earth abundant catalysts (rather than precious metal catalysts). Once developed, these synthetic protocols can be exploited directly by scientists at ParazaPharma Inc. in proprietary API synthesis/drug development. Success in this project will greatly accelerate the industrial partner's drug development program, thereby leading to more rapid identification of novel therapies to the benefit of all Canadians.