Momelotinib(1),a Janus kinase 1/2(JAK1/JAK2)inhibitor,was synthesized via a new synthetic route in three steps.The cyclization of ethyl 4-acetylbenzoate(2),N,N-dimethylformamide dimethyl acetal(DMF-DMA)and urea was achieved successfully to give ethyl 4-(2-oxo-1,2-dihydropyrimidin-4-yl)benzoate(3),which was subjected to the amination with 4-morpholinoaniline(4)in the presence of(benzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluorophosphate(PyBOP)and 1,8-diazabicyclo[5.4.0]undec-7-ene(DBU)to afford ethyl 4-[2-[(4-morpholinophenyl)-amino]pyrimidin-4-yl]benzoate(5).Compound 5 was subjected to the amidation with 2-aminoacetonitrile in the presence of air and potassium tert-butoxide to deliver the target product with purity of 99.5％.This new synthetic route had fewer reaction steps and high overall yield(70％based on 2).
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