The original synthesis of PKI-587 was a linear 5 step synthesis. One step was a Pd catalyzed Suzuki reaction and another used a low melting isocyanate, both of which we would like to avoid in an improved route. We also saw an opportunity to make the synthesis convergent. The talk will present the different chemistry we explored to achieve these goals.

Process development of the PI3K/mTOR inhibitor PKI-587

248th National Meeting (2014)

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