Potassium Phosphate, Tribasic → HCID 69732978, compound

Participants

Reaction Steps

A mixture of 3′-bromo-6′-(3-chloro-benzyloxy)-3,4,5,6-tetrahydro-2H-[1,2′]bipyrazinyl-4-carboxylic acid tert-butyl ester (I-3j) (82 mg, 0.17 mmol), methylboronic acid (15.3 mg, 0.25 mmol), K3PO4 (72 mg, 0.34 mmol), dppf (4.7 mg, 0.0085 mmol) and PdCl2dppf(CH2Cl2)2 (6.9 mg, 0.0085 mmol) in THF (anhydrous, 1.2 ml) under a nitrogen atmosphere was heated to reflux for 16 h. The reaction mixture was cooled to room temperature and filtered through a pad of silica gel, eluting with EtOAc-hexane (6:4). The filtrate was concentrated in vacuo. The residue was purified by preparative TLC (EtOAc-hexane 1:1) to provide 72 mg of the title compound I-3k (>99% yield).

Provenance & Evidence