4-(4-chlorophenyl)morpholine → HCID 89775937, compound

Participants

Reaction Conditions

Reaction Steps

8-Pyrido[2,3-b]pyrazin-7-yl-[1,2,4]triazolo[1,5-a]pyrazin-2-ylamine, 4-(4-chloro-phenyl)-morpholine (1.1 eq.), chloro[2-(dicyclohexylphosphino)-3,6-dimethoxy-2′-4′-6′-tri-i-propyl-1,1′-biphenyl]2-(2-aminoethyl)phenyl)Pd(II) (0.25 eq), 2-(dicyclohexylphosphino)-3,6-dimethoxy-2′-4′-6′-tri-i-propyl-1,1′-biphenyl; BrettPhos (0.25 eq.) are combined and suspended in t-butanol. The suspension is purged with N2 and lithium bis(trimethylsilyl)amide, (3 eq; 20% (ca 1.06M) solution in THF/ethylbenzene) is added. The vessel is sealed under N2 and heated to 65° C. for 2 h and then to 110° C. for 2 h. The mixture is filtered and concentrated. Purification via prep. HPLC gives the title compound.

Provenance & Evidence