Development of On‐DNA Cyclic Imide Synthesis for DNA Encoded Library Construction

Author:

Xue Lijun1,Zhou Sufang1,Wu Jing1,Duchemin Nicolas2,Chen Bingxin1,Zhang Jie1,Zhang Huanqing1,Yang Kexin3,Hu Yun Jin1ORCID

Affiliation:

1. Pharmaron (Ningbo) Technology Development Co., Ltd. No. 800 Bin-Hai 4th Road, Hangzhou Bay New Zone Ningbo 315336 China

2. Pharmaron UK, Ltd. Innovation Park West Cl, Hertford Rd Hoddesdon EN11 9FH UK

3. Pharmaron Beijing Co., Ltd. 6 Taihe Road, BDA Beijing 100176 China

Abstract

AbstractHere, we describe a novel method for the on‐DNA synthesis of cyclic imides, an important class of molecules that includes several well‐known medications. Significantly, the new method enabled on‐DNA synthesis under mild conditions with high conversions and a broad functional group tolerance, utilizing ubiquitous bifunctional amines and bis‐carboxylic acid, or alkyl halides, and therefore served as the linchpin for DNA encoded library (DEL) synthesis. The mechanism study of off‐DNA and on‐DNA chemical transformations revealed unique insights in contrast to conventional chemical transformation.

Funder

Pharmaron

Publisher

Wiley

Subject

Organic Chemistry,Molecular Biology,Molecular Medicine,Biochemistry

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