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Regiocontrolled Palladium-Catalyzed Arylative Cyclizations of Alkynols
Journal of the American Chemical Society ( IF 14.4 ) Pub Date : 2014-04-17 , DOI: 10.1021/ja5029028 Daishi Fujino 1 , Hideki Yorimitsu 1, 2 , Atsuhiro Osuka 1
Journal of the American Chemical Society ( IF 14.4 ) Pub Date : 2014-04-17 , DOI: 10.1021/ja5029028 Daishi Fujino 1 , Hideki Yorimitsu 1, 2 , Atsuhiro Osuka 1
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Tuning the reactivity of arylpalladium intermediates enables control of catalytic arylative 5-exo and 6-endo cyclizations of alkynols. The two modes of cyclizations represent a rare example of controllable, regioselective difunctionalization of alkynes. The cyclizations are useful in offering a divergent synthesis of oxygen-containing heterocycles, which is of synthetic use for further derivatization. Formal synthesis of an hNK-1 receptor antagonist also showcases the utility of our arylative cyclization.
中文翻译：
区域控制的钯催化的炔醇芳基环化
调节芳基钯中间体的反应性可以控制炔醇的催化芳基化 5-exo 和 6-endo 环化。这两种环化模式代表了炔烃可控、区域选择性双官能化的罕见例子。环化可用于提供含氧杂环的发散合成，其对于进一步衍生化具有合成用途。hNK-1 受体拮抗剂的正式合成也展示了我们芳基化环化的效用。
更新日期：2014-04-17
中文翻译：
区域控制的钯催化的炔醇芳基环化
调节芳基钯中间体的反应性可以控制炔醇的催化芳基化 5-exo 和 6-endo 环化。这两种环化模式代表了炔烃可控、区域选择性双官能化的罕见例子。环化可用于提供含氧杂环的发散合成，其对于进一步衍生化具有合成用途。hNK-1 受体拮抗剂的正式合成也展示了我们芳基化环化的效用。
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