一种从叔羧酸出发，构建受阻烷基氮杂环的通用一锅法。
A General One-Pot Protocol for Hindered -Alkyl Azaheterocycles from Tertiary Carboxylic Acids.
机构信息
Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States.
IDSU, WuXi AppTec Co., Ltd., Shanghai 200131, China.
出版信息
Org Lett. 2020 Jun 5;22(11):4180-4184. doi: 10.1021/acs.orglett.0c01254. Epub 2020 May 8.
In this letter, we report a general one-pot strategy that utilizes three elementary steps (decarboxylative hydrazination, Boc deprotection, and heterocycle condensation) to regioselectively prepare hindered C(sp) substituted pyrazoles and triazoles. The operational simplicity of this sequence and ubiquity of tertiary carboxylic acids allow rapid access to hindered -alkyl azaheterocycles that will be useful to practitioners of medicinal chemistry and agro-chemistry.
在这封信中，我们报告了一种通用的一锅法策略，该策略利用三个基本步骤（脱羧肼化、Boc 脱保护和杂环缩合）来区域选择性地制备受阻 C(sp)取代的吡唑和三唑。该序列的操作简单性和叔羧酸的普遍性允许快速获得受阻的 -烷基氮杂环，这对药物化学和农业化学的从业者将是有用的。
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