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- W2912176974 abstract "The original synthesis of the irreversible epidermal growth factor receptor (EGFR) T790 M inhibitor 1 was enabled by successful application of ammonium hydroxide to cleanly cleave the N-hydroxymethyl group and by development of high yielding conditions for the subsequent amidation reaction. Furthermore, a protection-free and regioselective new synthetic route was developed that shortened the synthesis from the original 8 steps to 6 steps and improved the overall yield from 5% to 34% on scale. Crystallizations of 1 and intermediates were correspondingly developed to control the quality en route." @default.
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- W2912176974 date "2019-01-31" @default.
- W2912176974 modified "2023-10-12" @default.
- W2912176974 title "Early Process Development of an Irreversible Epidermal Growth Factor Receptor (EGFR) T790 M Inhibitor" @default.
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- W2912176974 doi "https://doi.org/10.1021/acs.oprd.8b00437" @default.
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