| 摘要 |
Disclosed herein is a process for preparing an azaindole compound of Formula I, wherein the substituents are as defined in the specification. The process comprises reacting intermediates in water, organic solvents, a base, and a transition metal catalyst, wherein the organic solvents are selected from the group consisting of acetonitrile, toluene, N,N-dimethylformamide, N,N-dimethylacetamide, acetone, methyl tert-butyl ether, methanol, propanol, isopropanol, butanol, and tert-butanol. In a particular embodiment, the process produces compounds of Formula Ia [(R)-2-(2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-ylamino)-2-methyl-N-(2,2,2-trifluoroethyl)butanamide] and Ib [2-(2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)-2-methy-N-(2,2,2-trifluoroethy)propanamideand (Ib)]. The compounds of Formula I are useful as inhibitors of Janus kinases (JAK). |
