Abstract A process route for trans-4-(5-Bromo-2-chloro-pyrrolo[2,3-d]pyrimidin-7-yl)-cyclohexanol (1), the key intermediate for MER/FLT3 dual inhibitors is developed. The pivotal steps are to increase the selectivity of dechlorination in the first step, and to obtain pure trans-1 in the last step. With this process in hand, greater than 5 kg of pure trans-1 can be obtained in one batch.

Development of a multikilogram scale synthesis of trans-4-(5-bromo-2-chloro-pyrrolo[2,3-d]pyrimidin-7-yl)-cyclohexanol: A key intermediate for MER/FLT3 dual inhibitors

252nd National Meeting (2016)

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