Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa.
Department of Pharmaceutical Sciences, School of Pharmacy, Sefako Makgatho Health Sciences University, Pretoria 0204, South Africa.
Molecules. 2022 Oct 13;27(20):6850. doi: 10.3390/molecules27206850.
A simple, green, and highly efficient protocol for the synthesis of isocyanides is described. The reaction involves dehydration of formamides with phosphorus oxychloride in the presence of triethylamine as solvent at 0 °C. The product isocyanides were obtained in high to excellent yields in less than 5 min. The method offers several advantages including increased synthesis speed, relatively mild conditions, and rapid access to large numbers of functionalized isocyanides, excellent purity, increased safety, and minimal reaction waste. The new approach of synthesising dehydrative isocyanides from formamides is significantly more environmentally-friendly than prior methods.
描述了一种简单、绿色、高效的异氰酸酯合成方法。该反应涉及在三乙胺作为溶剂的存在下,用氧氯化磷使甲酰胺脱水,在 0°C 下进行。在不到 5 分钟的时间内,以高至优异的收率获得了产物异氰酸酯。该方法具有几个优点,包括提高的合成速度、相对温和的条件以及快速获得大量官能化异氰酸酯、优异的纯度、提高的安全性和最小的反应废物。与以前的方法相比,从甲酰胺合成脱水异氰酸酯的新方法具有显著的环境友好性。