An Amphiphilic Polymer-Supported Strategy Enables Chemical Transformations under Anhydrous Conditions for DNA-Encoded Library Synthesis was written by Ruff, Yves;Martinez, Roberto;Pelle, Xavier;Nimsgern, Pierre;Fille, Pascale;Ratnikov, Maxim;Berst, Frederic. And the article was included in ACS Combinatorial Science in 2020.Synthetic Route of C6H4INO2 This article mentions the following:
The use of DNA-encoded libraries has emerged as a powerful hit generation technol. Combining the power of combinatorial chem. to enumerate large compound collections with the efficiency of affinity selection in pools, the methodol. makes it possible to interrogate vast chem. space against biol. targets of pharmaceutical relevance. Thus, the chem. transformations employed for the synthesis of encoded libraries play a crucial role in the identification of diverse and drug-like starting points. Currently established transformations have mostly been limited to water-compatible reactions to accommodate the growing oligonucleotide tag. Herein, we describe the development of a practical catch-and-release methodol. utilizing a cationic, amphiphilic PEG-based polymer to perform chem. transformations on immobilized DNA conjugates under anhydrous conditions. We demonstrate the usefulness of our APTAC (amphiphilic polymer-facilitated transformations under anhydrous conditions) approach by performing several challenging transformations on DNA-conjugated small mols. in pure organic solvents: the addition of a carbanion equivalent to a DNA-conjugated ketone in THF, the synthesis of saturated heterocycles using the tin (Sn) amine protocol (SnAP) in dichloromethane, and the dual-catalytic (Ir/Ni) metallaphotoredox decarboxylative cross-coupling of carboxylic acids to DNA-conjugated aryl halides in DMSO. In addition, we demonstrate the feasibility of the latter in multititer-plate format. In the experiment, the researchers used many compounds, for example, 5-Iodonicotinic acid (cas: 15366-65-1Synthetic Route of C6H4INO2).
5-Iodonicotinic acid (cas: 15366-65-1) belongs to iodide derivatives. Organic iodides are organic compounds containing a carbon-iodine (C-I) bond. The carbon-iodine bond is weaker than other carbon-halogen bonds due to the poor electronegative nature of the iodine atom. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.Synthetic Route of C6H4INO2
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com