Gupta Anjali, Laha Joydev K
Department of Pharmaceutical Technology (Process Chemistry), National Institute of Pharmaceutical Education and Research, S. A. S. Nagar, Punjab 160062, India.
Org Lett. 2024 Nov 22;26(46):10013-10019. doi: 10.1021/acs.orglett.4c03870. Epub 2024 Nov 6.
A new approach for direct formylation of various amines has been disclosed using a novel formylating agent, formylhydrazine, to afford -formylamines in significant yields with application in the gram-scale synthesis of chlorothiazide. This transformylation (transfer of a formyl group from hydrazine to amines) occurs via denitrogenation in the presence of KSO as the exclusive reagent with water as the solvent. Two reaction pathways involving extremely underexplored formyl or hemiaminal radicals have been postulated, which require further investigation.
已经公开了一种使用新型甲酰化剂甲酰肼对各种胺进行直接甲酰化的新方法，能够以可观的产率得到甲酰胺，并应用于克级规模合成氯噻嗪。这种甲酰基转移反应（将甲酰基从肼转移到胺上）是在以水为溶剂、仅使用KSO作为试剂的情况下通过脱氮作用发生的。已经推测出两条涉及极少被研究的甲酰基或半胺基自由基的反应途径，这需要进一步研究。
