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Published on: July 6, 2016
High-yield and high-purity amide bond formation using DMTMM PF6 for DNA-encoded libraries
Takumi Hosozawa1, Masatoshi Niwa1, Hisayuki Takeuchi1
1Pharmaceutical Research Department, Chemical Research Laboratories, Nissan Chemical Corporation, 10-1, Tsuboi-Nishi 2-chome, Funabashi, Chiba, Japan.
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.
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