反应详情

A solution of 4-chloro-6-pyridin-3-yl-2-pyridin-2-yl-pyrimidine (Intermediate A) (1 eq, 0.2 g), C-(1H-indol-4-yl)-methylamine (1.1 eq, 0.12 g) and K2CO3 (3 eq, 0.308 g) in NMP (6 ml) is heated using microwave radiation at 120° C. for 1 hour. After cooling to room temperature, the mixture is partitioned between EtOAc/water and the organic portion is separated, washed with brine, dried (MgSO4) and concentrated in vacuo. The crude residue is purified by mass directed preparative HPLC eluting with acetonitrile in water—0.1% TFA and the appropriate fractions are combined and concentrated in vacuo. The resulting residue is loaded onto a SCX-2 cartridge eluting with MeOH followed by 2M NH3 in MeOH. The methanolic ammonia fractions are concentrated in vacuo and dried under vacuum to afford the title compound [M+H]+=379.

1. customat 120° C.
2. customfor 1 hour
3. customthe mixture is partitioned between EtOAc/water
4. customthe organic portion is separated
5. washwashed with brine
6. dry with materialdried (MgSO4)
7. concentrationconcentrated in vacuo
8. customThe crude residue is purified by mass
9. washeluting with acetonitrile in water—0.1% TFA
10. concentrationconcentrated in vacuo
11. washeluting with MeOH
12. concentrationThe methanolic ammonia fractions are concentrated in vacuo
13. customdried under vacuum