Development of carbon monoxide surrogates for chemical synthesis

此次合作的主要目标是利用最近发现的羧基mida -硼酸盐（CMB），在一系列小分子支架中针对特定位点引入标记碳。我们的合作伙伴Merck和Eurofins Alphora将主要使用CMB进行含杂环药物先导物的标记研究。Yudin小组最近证明了CMB的合成，CMB是合成富杂原子硼化杂环的稳定的c1构建块。这项技术受到专利申请的保护。我们将与Merck & Co.和Eurofins Alphora合作，扩大CMB的合成潜力。这次合作将集中于探索通过羰基化转化来细化酰基部分的众多机会。实现我们目标的努力将依赖于默克公司提供的高通量实验（HTE）技术。尽管在学术研究中将Co纳入交叉耦合转化的重要性，但羰基化在工业HTE中的应用很少。这些发现将对总部位于安大略省的Eurofins Alphora（该基金的另一个合作伙伴）具有巨大价值。在我们为博士和硕士毕业生寻找就业机会的这一充满挑战的时刻，我们与Eurofins alpha的关系尤为重要。通过继续与默克公司和欧睿的合作，我们将让学生在学术研究的早期阶段就在专业的环境中发展，并探索在上述公司的短期实习机会。这将导致在毕业后有资格进入加拿大劳动力市场的高素质人才数量的增加，从而有利于加拿大制药技术部门的整体增长。

The main goal of this partnership is to leverage the recently discovered carboxy-MIDA-boronate (CMB) toward site-specific introduction of labelled carbon in a range of small molecule scaffolds. Our partners - Merck and Eurofins Alphora - will primarily use CMB for labelling studies of heterocycle-containing drug leads. The Yudin group recently demonstrated the synthesis of CMB, which is a bench-stable C1-building block for the synthesis of heteroatom-rich borylated heterocycles. This technology has been protected by a patent application. In partnership with Merck & Co. and Eurofins Alphora we will expand the synthetic potential of CMB. This collaboration will be focused on exploring the numerous opportunities for the elaboration of the acyl moiety via carbonylative transformations. Efforts towards achieving our goals will rely on the high-throughput experimentation (HTE) technology provided by Merck & Co. Despite the prominence of incorporating CO in cross-coupling transformations in academic research, carbonylation has found only sparse application in industrial HTE. These findings will be of tremendous value to the Ontario-based Eurofins Alphora, the other partner on this grant. Our relationship with Eurofins Alphora is particularly significant at this challenging time as we pursue employment opportunities for the PhD and MSc graduates. By continuing our collaboration with Merck and Eurofins Alphora we will allow students to develop in a professional environment at early stages in their academic studies, and to explore short-term placements in the aforementioned companies. This will lead to the increase in amount of highly qualified personnels that are eligible to enter Canada's workforce upon graduation, thereby benefiting the overall growth of the Canadian pharmaceutical technology sector.