A facile synthetic route for antineoplastic drug GDC-0449
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AbstractIn the current study a facile synthetic route for preparing antineoplastic drug GDC-0449 is investigated. Starting with pyridine-1-oxide and 1-iodo-3-nitrobenzene, the intermediate product 2-(2-chloro-5-nitrophenyl) pyridine was prepared by cross-coupling, deoxidation and halogenation. The final compound was then synthesised by reduction of the nitro group followed by amidation. This synthetic route avoids the use of unstable organometallic or organic boride compounds; it employs relatively inexpensive and bench-stable reagents, involves readily controllable reaction conditions, and achieves a relatively high yield.
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2016 ◽
Vol 12
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pp. 835-845
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2020 ◽
2018 ◽
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1992 ◽
Vol 57
(2)
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pp. 393-396
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2012 ◽
Vol 2012
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pp. 1-9
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2017 ◽
Vol 41
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pp. 168-171
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2009 ◽
Vol 48
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pp. 1351-1351
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Vol 2007
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pp. 486-489
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