Tetrahydrofuran → (5-Chloro-7-morpholinothiazolo[4,5-d]pyrimidin-2-yl)(4-methylsulfonylpiperazin-1-yl)methanone

Participants

Reaction Conditions

Reaction Steps

4-(5-Chloro-2-iodothiazolo[4,5-d]pyrimidin-7-yl)morpholine 27 was dissolved in tetrahydrofuran and combined with triethylamine, 1-methylsulfonylpiperazine hydrochloride (2 eq), and trans-dichlorobis(triphenylphosphine)palladium(II) (0.1 eq). The solution was flushed with carbon monoxide stirred under a carbon monoxide balloon at 55° C. overnight. The solution was cooled to room temperature. Water was added and the solution was filtered to yield the tan product of (5-chloro-7-morpholinothiazolo[4,5-d]pyrimidin-2-yl)(4-methylsulfonylpiperazin-1-yl)methanone.

Provenance & Evidence