Synthetic Communications p. 1169 - 1174 (2017)
Update date:2022-08-29
Topics:
Yu, Qian-Ying
Zeng, Huang
Yao, Kai
Li, Jian-Qi
Liu, Yu
A novel and practical strategy for the synthesis of vonoprazan fumarate 1, a novel potassium-competitive acid blocker, has been developed. Vonoprazan fumarate was obtained through a four-step process starting from 5-(2-fluorophenyl)-1H-pyrrole-3-carboxylate and including ester hydrolyzing, methylamine substitution, sulfonyl chloride substitution, and amide reduction. Key to the strategy is the amide reduction taking a novel and practical protocol. The main advantages of this route include two parts: controllable impurity and acceptable overall yield.
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