反应详情

A mixture of pyrazin-2-amine (12) (1.1 eq.), 2-(4-formylphenoxy)-N-methylacetamide (9) (1.1 eq.) and a catalytic amount of Sc(OTf)3 was stirred in 2 mL of 1:1 DCM/MeOH at room temperature for 30 minutes. To this was added 5-isocyano-2,3-dihydroinden-1-one O-tert-butyldimethylsilyl oxime (1 eq.) as a 2 mL solution in 1:1 DCM/MeOH and the mixture was stirred at room temperature for 18 hours. The reaction mixture was then concentrated under vacuum and the residue taken up in EtOAc (with a small amount of methanol added to help with dissolution) and purified by column using 1-5% MeOH/EtOAc+1% NH4OH. The desired product (14) was isolated as a light yellow solid. MS (APCI) m/z 443.1 (M+1).

1. concentrationThe reaction mixture was then concentrated under vacuum
2. additionadded
3. dissolutionto help with dissolution) and
4. custompurified by column