Li Wanyong, Lv Mengting, Luo Xiaolin, Wang Zhouyu, Song Qiao, Yu Xiaoqi
Department of Chemistry, Xihua University Chengdu 610039 China
Asymmetric Synthesis and Chiral Technology Key Laboratory of Sichuan Province Yibin 644000 China.
RSC Adv. 2024 Jul 1;14(29):20656-20659. doi: 10.1039/d4ra03683b. eCollection 2024 Jun 27.
In the quest for sustainable and efficient synthetic methodologies within medicinal chemistry, the synthesis of carbamates and their derivatives holds a pivotal role due to their widespread application in bioactive compounds. This investigation unveils a novel methodology for the straightforward transformation of Boc-protected amines into carbamates, thiocarbamates, and ureas, utilizing -butoxide lithium as the sole base. This approach effectively obviates the necessity for hazardous reagents and metal catalysts, presenting marked enhancements compared to traditional synthetic pathways. Notably, the method demonstrates facile scalability to gram-level production. This study contributes to the advancement of sustainable synthetic methodologies, offering a more benign and efficient alternative for the synthesis of key chemical intermediates with implications for broad pharmaceutical and agrochemical applications.
在药物化学领域寻求可持续且高效的合成方法时,氨基甲酸酯及其衍生物的合成因其在生物活性化合物中的广泛应用而具有关键作用。本研究揭示了一种新颖的方法,该方法以叔丁醇锂作为唯一碱,可将Boc保护的胺直接转化为氨基甲酸酯、硫代氨基甲酸酯和脲。这种方法有效避免了使用危险试剂和金属催化剂的必要性,与传统合成途径相比有显著改进。值得注意的是,该方法可轻松扩展至克级生产。这项研究推动了可持续合成方法的发展,为关键化学中间体的合成提供了一种更安全、高效的替代方法,对广泛的制药和农用化学品应用具有重要意义。