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The Wittig–Horner reaction for the synthesis of neratinib

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Abstract

The Wittig–Horner reaction is a classic method to get alkenes by reaction phosphonates with carbonyl compounds. In this study, it was used for the synthesis of the anticancer drug neratinib. In this method, ethyl diethoxyphosphinylacetate and dimethylaminoacetaldehyde diethylacetal, replacing (E)-4-(dimethylamino)but-2-enoyl acid hydrochloride and oxalyl chloride, were used to synthesize the 6-position side chain of neratinib.

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Acknowledgments

This work was supported by National Basic Research Program of China (No. 2011CB933503).

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Correspondence to Yang Chen or Min Ji.

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Gu, N., Yang, J., Wang, P. et al. The Wittig–Horner reaction for the synthesis of neratinib. Res Chem Intermed 39, 3105–3110 (2013). https://doi.org/10.1007/s11164-012-0822-4

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  • DOI: https://doi.org/10.1007/s11164-012-0822-4

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