High-yield and high-purity amide bond formation using DMTMM PF6 for DNA-encoded libraries

被引：1
作者：
Hosozawa, Takumi [1 ]
Niwa, Masatoshi [1 ]
Takeuchi, Hisayuki [1 ]
Inohana, Takehiko [1 ]
Okumura, Kaori [1 ]
Itoh, Shin [1 ]
机构：
[1] Nissan Chem Corp, Chem Res Labs, Pharmaceut Res Dept, 10-1 Tsuboi Nishi 2 Chome, Funabashi, Chiba, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2024年 / 110卷
关键词：
DNA-encoded libraries (DELs); Amidation reaction; Sterically hindered amines and carboxylic acids; DMTMMPF6; on-DNA;
D O I：
10.1016/j.bmcl.2024.129859
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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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页数：5
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