Methods for the synthesis of 5,6,7,8-tetrahydro-1,8-naphthyridine fragments for alphaVbeta3 integrin antagonists |
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| Authors: | Hartner Frederick W Hsiao Yi Eng Kan K Rivera Nelo R Palucki Michael Tan Lushi Yasuda Nobuyoshi Hughes David L Weissman Steven Zewge Daniel King Tony Tschaen Dave Volante R P |
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| Institution: | Department of Process Research, Merck Research Laboratories, Rahway, NJ 07065, USA. fred_hartner@merck.com |
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| Abstract: | The preparation of 3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propan-1-amine 2a and 3-(7R)-7-methyl-5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl]propan-1-amine 2b, key intermediates in the synthesis of alpha(V)beta(3) antagonists, is described. The syntheses rely on the efficient double Sonogashira reactions of 2,5-dibromopyridine 3 with acetylenic alcohols 4a/4b and protected propargylamines 10a-e followed by Chichibabin cyclizations of 3,3'-pyridine-2,5-diyldipropan-1-amines 9a/9b. |
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