A palladium-catalysed direct arene C–H fluoroalkoxylation of 4-aryl-pyrrolo[2,3-d]pyrimidine derivatives with fluorinated alcohols is described. Highly site-selective mono- or bis-fluoroalkoxylation can be achieved by tuning the reaction conditions, affording various fluoroalkoxylated pyrrolo[2,3-d]pyrimidine derivatives in moderate to good yields, which offer rational tailoring of their biological activity for their application in the field of pharmaceutical chemistry.
![Graphical abstract: Palladium-catalysed site-selective arene ortho C–H fluoroalkoxylation of 4-aryl-pyrrolo[2,3-d]pyrimidines](http://hg.y866.cn/compound/lib/scimg/usr/1/D3OB00084B.jpg)