Processes and intermediates for producing azaindoles

    公开(公告)号:NZ619699A

    公开(公告)日:2016-03-31

    申请号:NZ61969912

    申请日:2012-07-03

    Applicant: VERTEX PHARMA

    Abstract: 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).

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