Reaction equation
C1CCNC1.COc1cc(N2CCN(C(C)=O)CC2)ccc1Nc1ncc(Cl)c(-c2cnc3cc(Cl)ccn23)n1>CC(C)(C)[O-].CC(C)c1cc(C(C)C)c(-c2ccccc2P(C2CCCCC2)C2CCCCC2)c(C(C)C)c1.COc1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.[Na+].[Pd].[Pd]>COc1cc(N2CCN(C(C)=O)CC2)ccc1Nc1ncc(Cl)c(-c2cnc3cc(N4CCCC4)ccn23)n1Participants
Reactant 2
Product 1
Reagents, catalysts & solvents 4
Conditions
- Temperature
- 105 °C
Procedure
_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 _ _ _
Sources & evidence
- ORD record
- ord-89a1182c94f742baabcda9e64ef54d27
- Source dataset
- 750 AstraZeneca ELN dataset
- Original link
- View source
Linked notes
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