Takumi Hosozawa; Masatoshi Niwa; Hisayuki Takeuchi; Takehiko Inohana; Kaori Okumura; Shin Itoh
Bioorg. Med. Chem. Lett., 2024, 129859
https://doi.org/10.1016/j.bmcl.2024.129859

Abstract

In this study, we report on the ability of DMTMM PF6 to improve the amidation reaction. The on-DNA amidation reaction using DMTMM PF6 demonstrates higher conversion rates than those using HATU or DMTMM Cl, particularly with challenging sterically hindered amines and carboxylic acids. The developed method enables the expansion of available building blocks and the efficient synthesis of high-purity DNA-encoded libraries.