The latest research shows that oxalyl chloride monoethyl ester, as a highly selective acylation reagent, can achieve efficient reactions under mild conditions in the synthesis of pharmaceutical intermediates such as nitrogen-containing heterocycles and amino acid esters. The by-products are easy to separate and the atomic economy is improved, addressing the shortcomings of traditional acylation reagents, which are highly corrosive and generate a lot of waste. It has completed kilogram-scale verification and promotes the green upgrade of drug synthesis processes.