Journal
ORGANIC LETTERS
Volume 21, Issue 15, Pages 6112-6116Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.9b02259
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Funding
- Croucher Foundation
- DARPA Make-It program [ARO W911NF-16-2-0023]
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A modular continuous flow synthesis of imatinib and analogues is reported. Structural y diverse imatinib analogues are rapidly generated using three readily available building blocks via a flow hydration/chemoselective C-N coupling sequence. The newly developed continuous flow hydration and amidation modules each exhibit a broad scope with good to excellent yields. Overall, the method described does not require solvent switches, in-line purifications, or packed-bed apparatuses due to the judicious manipulation of flow setups and solvent mixtures.
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