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- W3040331391 abstract "The process selection and subsequent development of a reliable, scalable synthesis of the anticancer prodrug tirapazamine (SR259075) is described in this paper. Reaction of benzofuroxan with cyanamide in acetonitrile in the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene at 20–25 °C afforded, after an acidic workup, the targeted molecule in good yield at a kilogram scale. Notable critical parameters and safety enhancements are defined and successfully implemented to produce three consecutive validation batches in a reproducible manner." @default.
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- W3040331391 date "2020-07-01" @default.
- W3040331391 modified "2023-09-30" @default.
- W3040331391 title "Development and Validation of a Kilogram-Scale Synthesis of Tirapazamine" @default.
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- W3040331391 doi "https://doi.org/10.1021/acsomega.0c01250" @default.
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