GlaxoSmithKline, Cancer Research, Protein Dynamics Discovery Performance Unit, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.
Org Lett. 2012 Aug 3;14(15):3906-8. doi: 10.1021/ol301655f. Epub 2012 Jul 18.
A simple, novel, and efficient route for the synthesis of 5-amino-3-aryl-1-(tert-butyl)-1H-pyrazole-4-carboxamides 1 has been devised. Preparation of pyrazole bromide 3 from potassium tricyanomethanide can be accomplished in only two steps in good yield and features a selective Sandmeyer reaction on the corresponding diaminopyrazole. This allows for a more versatile synthesis of 5-amino-3-aryl-1-(tert-butyl)-1H-pyrazole-4-carboxamides 1 than was previously possible.
已经设计出一种合成 5-氨基-3-芳基-1-(叔丁基)-1H-吡唑-4-甲酰胺 1 的简单、新颖且高效的路线。从氰基三氟甲烷钾制备吡唑溴 3 可以在两步中以良好的产率完成，并且在相应的二氨基吡唑上具有选择性的Sandmeyer 反应。这使得比以前更通用的合成 5-氨基-3-芳基-1-(叔丁基)-1H-吡唑-4-甲酰胺 1 成为可能。
