钯催化的酰腙的化学选择性单芳基化反应在[1,2,4]三唑并[4,3-a]吡啶合成中的应用。
Palladium-catalyzed chemoselective monoarylation of hydrazides for the synthesis of [1,2,4]triazolo[4,3-a]pyridines.
机构信息
Department of Medicinal Chemistry, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799, USA.
出版信息
Org Lett. 2010 Feb 19;12(4):792-5. doi: 10.1021/ol902868q.
PMID:20099864
Abstract
An efficient and convenient method for the synthesis of [1,2,4]triazolo[4,3-a]pyridines was exemplified by the synthesis of 20 analogues bearing a variety of substituents at the 3-position. The methodology involves a palladium-catalyzed addition of hydrazides to 2-chloropyridine, which occurs chemoselectively at the terminal nitrogen atom of the hydrazide, followed by dehydration in acetic acid under microwave irradiation.
摘要
一种高效便捷的合成[1,2,4]三唑并[4,3-a]吡啶的方法，通过合成 20 个具有不同取代基的 3-位取代物的类似物来举例说明。该方法涉及钯催化酰腙与 2-氯吡啶的加成，该反应在酰腙的末端氮原子上发生化学选择性加成，然后在微波辐射下在乙酸中脱水。
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