Pyrrolidine → 1-(4-(4-(5-Chloro-4-(7-(pyrrolidin-1-yl)imidazo[1,2-a]pyridin-3-yl)pyrimidin-2-ylamino)-3-methoxyphenyl)piperazin-1-yl)ethanone

関与物質

反応条件

反応手順

_pyrrolidine (0.025 mL, 0.30 mmol)_ _was added to a suspension of_ _1-(4-(4-(5-chloro-4-(7-chloroimidazo[1,2-a]pyridin-3-yl)pyrimidin-2-ylamino)-3-methoxyphenyl)piperazin-1-yl)ethanone (104 mg, 0.20 mmol)_ _ in __dioxane (3.5 mL)_ _, followed by_ _sodium 2-methylpropan-2-olate (58.5 mg, 0.61 mmol)_ _, the mixture was degassed by bubbling N2 through , then a solution of pre-activated ( 50°C /15 min ) solution in dioxanne (1 ml) of __dicyclohexyl(2',4',6'-triisopropylbiphenyl-2-yl)phosphine (7.26 mg, 0.02 mmol)_ _( Xphos) and_ _TRIS(DIBENZYLIDENEACETONE)DIPALLADIUM (4.65 mg, 5.07 µmol)_ _was added ._ _The brown-orange suspension was stirred at _ _105 °C_ _1 hr ( trace of reaction )_ _anisole (2 mL)_ _was added and then overnight under nitrogen atmosphere : few of reaction observed from 1 hr to 16 hrs heating_ _and TBAC ( 25 mg ) were added and the heating was continued overnight no reaction _ _ _

情報源と証拠