Organic Process Research & Development 2018-03-29

Exemplifying Prediction of Preferred Coupling Partners in Developing a Buchwald–Hartwig Coupling for the Synthesis of a c-Kit Inhibitor

Quanbing Wu, Xin Xiong, Yudong Cao, Lijuan He, Zhongbo Fei

Index: 10.1021/acs.oprd.8b00043

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Abstract

Two convergent syntheses for compound 1 are described that apply Buchwald–Hartwig coupling as the key step. This development work provides a direct comparison of the coupling results from different coupling partners and illustrates that more efficiency can be achieved by selecting the right coupling partners.