通过涉及锌化哒嗪-3(2H)-酮的 Negishi 反应合成（杂）芳基哒嗪-3(2H)-酮。
Synthesis of (hetero)arylated pyridazin-3(2H)-ones via Negishi reaction involving zincated pyridazin-3(2H)-ones.
机构信息
Organic Synthesis, Department of Chemistry, University of Antwerp, Groenenborgerlaan 171, B-2020 Antwerp, Belgium.
出版信息
J Org Chem. 2011 Dec 2;76(23):9648-59. doi: 10.1021/jo201587j. Epub 2011 Nov 9.
PMID:22017314
Abstract
Zincated pyridazin-3(2H)-ones generated via bromine-magnesium exchange followed by transmetalation using ZnCl(2) or via lactam-directed ortho C4-H zincation with TMPZnCl·LiCl have been synthesized. These in situ created organometallics can be used in Negishi reactions with iodo(hetero)arenes delivering a new approach toward (hetero)arylpyridazin-3(2H)-ones.
摘要
通过溴-镁交换生成锌化吡啶并[3,2-d]嘧啶-3(2H)-酮，然后用 ZnCl(2)进行转金属化，或通过内酰胺导向的邻位 C4-H 锌化与 TMPZnCl·LiCl 生成锌化吡啶并[3,2-d]嘧啶-3(2H)-酮，已被合成。这些原位生成的有机金属试剂可以用于 Negishi 反应与碘（杂）芳烃反应，为（杂）芳基吡啶并[3,2-d]嘧啶-3(2H)-酮的合成提供了一种新方法。
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