A synthetic route for vornolazan fumarate was provided. The process begins with 5-(2-fluorophenyl)-1H-pyrrole-3-carboxaldehyde, which undergoes N-sulfonation to form intermediate 15-(2-fluorophenyl)-1-(pyridine-3-sulfonyl)-1H-pyrrole-3-carboxaldehyde. The intermediate is then reacted with a sodium triacetoxyboride aqueous solution via ammoniation and reduction to yield vornolazan. The final product was obtained by salting vornolazan with fumaric acid, yielding crude vornolazan fumarate, which is purified to achieve the desired purity. The overall yield is 55% (based on starting materials), with a liquid-phase purity of 99.72%, meeting all relevant quality standards. The synthesis method is simple to operate, produces high-purity products with minimal impurities, and utilizes readily available raw materials, making it suitable for industrial-scale production.
刘晓莲. 富马酸沃诺拉赞合成工艺研究[J]. 煤炭与化工, 2026, 49(1): 125-128,132..
Liu Xiaolian. Research on the synthesis process of vonoprazan of fumarate. CCI, 2026, 49(1): 125-128,132..