The Palladium-Catalyzed Cross-Coupling Reaction of Phenylboronic Acid with Haloarenes in the Presence of Bases

Towards the evaluation in an animal disease model: Fluorinated 17β-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme

“…III was reacted with 4-aminophenylboronic acid pinacol ester in a Suzuki cross coupling reaction [43] to afford the final compound 1. Compounds 2 and 30 were prepared from I and II, respectively, using the same methods as for 1 but in reversed order because the intermediates 2a and 30a were needed as starting materials in the syntheses according to scheme 2, vide infra.…”

Inhibition of 17β-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker

“…[33] FriedelCrafts acylation of the resulting intermediate 1a [34] with the appropriate benzoic acid chloride gave access to compounds 1-4.…”

Chlorophenols in organic synthesis

“…Palladium-catalyzed reactions of organic boron compounds with arylclorides are one of common synthetic methods for forming new carbon-carbon bonds [3]. Organic boron reagents are readily available, stable to air and non-reactive to various active fragments for which usually the protective groups introduction requires.…”