Development of carbon monoxide surrogates for chemical synthesis

这一合作伙伴关系的主要目标是利用最近发现的羧基-MIDA-硼酸酯(CMB)在一系列小分子支架中特定位置地引入标记碳。我们的合作伙伴默克和Eurofins Alphora将主要使用CMB进行含有杂环的药物先导的标记研究。玉丁基团最近证明了CMB的合成，这是一种用于合成富杂原子的硼化杂环的稳定的C1构筑块。这项技术已经受到专利申请的保护。我们将与默克公司和Eurofins Alphora合作，扩大中巴的合成潜力。这一合作将侧重于探索通过羰化转化精制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一氧化碳引入交叉偶联转化，但在工业高通量实验(HTE)中只发现了少量的应用。这些发现将对安大略省的Eurofins Alphora具有巨大的价值，该基金会是这笔赠款的另一个合作伙伴。在我们为博士和硕士毕业生寻找就业机会的这个充满挑战的时刻，我们与Eurofins Alphora的关系尤其重要。通过继续与默克和Eurofins Alphora的合作，我们将允许学生在学术学习的早期阶段在专业环境中发展，并探索在上述公司的短期就业机会。这将导致毕业后有资格进入加拿大劳动力大军的高素质人员数量增加，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.