3,4-二氢吡嗪并[1,2-b]吲唑及其6-氧化物的高效无痕固相合成
Efficient traceless solid-phase synthesis of 3,4-dihydropyrazino[1,2-b]indazoles and their 6-oxides.
作者信息
Pudelová Nadezda, Krchnák Viktor
机构信息
Department of Chemistry and Biochemistry, 251 Nieuwland Science Center, University of Notre Dame, Notre Dame, Indiana 46556, USA.
出版信息
J Comb Chem. 2009 May-Jun;11(3):370-4. doi: 10.1021/cc800181y.
Abstract
A highly efficient novel traceless solid-phase synthesis of 3,4-dihydropyrazino[1,2-b]indazoles and their 6-oxides was developed by using commercially available building blocks, diamines, 2-nitrobenzenesulfonyl chlorides, and bromoketones/bromoacetates. Mild reaction conditions, diversely substituted building blocks, and high purity of crude products enabled effective combinatorial syntheses of libraries.
摘要
利用市售的起始原料、二胺、2-硝基苯磺酰氯和溴代酮/溴代乙酸酯，开发了一种高效的新型无痕固相合成3,4-二氢吡嗪并[1,2-b]吲唑及其6-氧化物的方法。温和的反应条件、多样取代的起始原料以及粗产物的高纯度使得能够有效地组合合成文库。
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