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Efficient Synthesis of 4-Amino-2-methoxy-7,8-dihydropyrido[4,3-d]pyrimidin-5-ones: Practical Access to a Novel Chemotype in the Development of DGAT-1 Inhibitors

  作者 BAHNCK KEVIN B; SHAVNYA ANDREI; TAO YONG; LILLEY SUSAN C; ANDREWS MELISSA P; ASPNES GARY E; BERNHARDSON DAVID J; BILL DAVID R; BUNDESMANN MARK W; DOW ROBERT L; KARKI KAPIL; LE TUNG; LI QIFANG; MUNCHHOF MICHAEL J; NEMATALLA ASAAD; NIHLAWI MOHAMMED; PATEL LEENA; PERREAULT CHRISTIAN; WALDO MICHAEL  
  选自 期刊  Synthesis;  卷期  2012年44-20;  页码  3152-3157  
  关联知识点  
 

[摘要]A practical access to an unprecedented, fused bicyclic 4-amino-2-alkoxy-7,8-dihydropyrido[4,3-d]pyrimidin-5-one scaffold is developed. The synthesis of the potent inhibitor, 2-{4-[4-amino-2-methoxy-5-oxo-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl]phenyl}-2-methylpropanamide is detailed, with particular emphasis placed on synthetic efficiency and scalability. With the isolation of solid intermediates, the routes described offer clear elements of practicality and facilitate production of the target compound on large scale (>10 g) without chromatography.

 
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