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2.1.1 Amidation with Carboxylic Acids

DOI: 10.1055/sos-SD-241-00002

Li, Y.; Fang, X.; Wang, Y.Science of Synthesis: DNA-Encoded Libraries, (202418.

The latest data shows that the number of carboxylic acids available for purchase is 59 000, but only 24 000 meet the criteria for a “good” building block[‌1‌] [“rule of two” (Ro2)[‌2‌]]. A good-quality building block for medicinal chemistry could be defined as one typically having a molecular weight no greater than 200 Da, a clogP of less than 2 units, and no more than two hydrogen-bond donors and four hydrogen-bond acceptors. Over 20 000 carboxylic acids are available from commercial sources at a moderate cost of less than $150 per gram.[‌3‌]