2-Thiopheneboronic acid → (R)-2-(2-chloro-5-(2-thienyl)pyrimidine-4-ylamino)butan-1-ol

Participants

Reaction Steps

In the reaction of (R)-2-(2-chloro-5-bromopyrimidine-4-ylamino)butan-1-ol (18.17 g, 64.8 mmol) with thiophen-2-boronic acid (e. g.: Aldrich, Acros, Apin) (9.12 g, 128.0 mmol) according to procedure 3, the desired product is obtained in 71% yield (13.1 g) after chromatographic purification (silica gel, ethyl acetate/hexane (20%-50% ethyl acetate)).

Provenance & Evidence