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- W2085842707 abstract "Process development and salt selection for a novel VEGFR inhibitor are described. The overall convergent synthesis involved coupling of three key fragments, 2-chloronicotinoyl chloride, 4-isopropyl-3-methylaniline and 7-aminoisoquinoline. A cost-effective and scalable synthesis of 7-aminoisoquinoline was also achieved. A transition-metal-free S<sub>N</sub>Ar process enabled the final C–N coupling to afford the target molecule. A phosphate form of the drug substance with improved physical properties was selected for further development and the corresponding crystallization process was subsequently developed. Overall, a robust six-step route was developed and demonstrated on multikilogram scales affording the target compound in >30% yield and high purity (>99%)." @default.
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- W2085842707 date "2012-11-16" @default.
- W2085842707 modified "2023-10-18" @default.
- W2085842707 title "Development of a Scalable Synthesis of a VEGFR Inhibitor" @default.
- W2085842707 doi "https://doi.org/10.1055/s-0032-1317554" @default.
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