A practical synthesis of 2-((1H-pyrrolo[2,3-b]pyridine-4-yl)methylamino)-5- fluoronicotinic acid |
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Authors: | Wang Xin Zhi Ben Baum Jean Chen Ying Crockett Richard Huang Liang Eisenberg Shawn Ng John Larsen Robert Martinelli Mike Reider Paul |
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Institution: | Chemical Process R & D, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799, USA. xinw@amgen.com |
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Abstract: | A practical synthesis of a key pharmaceutical intermediate, 2-(1H-pyrrolo2,3-b]pyridine-4-yl)methylamino]-5-fluoronicotinic acid (1), is described. To introduce the aminomethyl moiety of 2 via a palladium-catalyzed cyanation/reduction sequence, a regioselective chlorination of 7-azaindole via the N-oxide was developed. A highly selective monodechlorination of 2,6-dichloro-5-fluoronicotinic acid was discovered to afford the nicotinic acid 3. The two building blocks 2 and 3 were then coupled to complete the preparation of 1. |
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