Organic lettersToll-Like Receptor 7Molecular StructureAlkylationToll-Like Receptor 8Pyrimidines
Scalable Synthesis of a Dual TLR7/8 Agonist via Highly Selective N2-Alkylation of 1H-Pyrazolo[4,3-d]pyrimidine.
Kai-Jiong Xiao, Yingju Xu, Lu Chen, Zheng Wu, Wenzhi Fang, Steven P Miller, Jingjun Yin
Published: 202510.1021/acs.orglett.5c04092
Abstract
We report a scalable synthesis of a potent dual TLR7/8 agonist featuring a pyrazolopyrimidine core. An acid-mediated selective N2-alkylation of 1H-pyrazolo[4,3-d]pyrimidine with free benzyl alcohol furnishes the N2-alkylated product in 72% yield with…
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