Regioselective Synthesis of 1-Alky I- or 1-Aryl-1H-indazoles via Copper-Catalyzed Cyclizations of 2-Haloarylcarbonylic Compounds

Dolores Vina; Esther del Olmo; Jose L.Lopez-Perez

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Regioselective Synthesis of 1-Alky I- or 1-Aryl-1H-indazoles via Copper-Catalyzed Cyclizations of 2-Haloarylcarbonylic Compounds

机译：通过2-卤代芳基羰基化合物的铜催化环化反应，区域选择性合成1-烷基I-或1-芳基-1H-吲唑

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A general method for the one-step regioselective synthesis of 1-alkyl- or 1-aryl-1H-indazoles from ortho-halogenated alkanoylphenones,benzophenones,and arylcarboxylic acids,via copper-catalyzed amination,was developed by using 0.2% mol of CuO in the presence of K2CO3.The reaction involves amination followed by intramolecular dehydration.Different functionalized alkyl aryl ketones,diaryl ketones,and benzoic acid derivatives were efficiently coupled with several hydrazines.Ligands commonly employed as catalysts for intermolecular amination were shown to be ineffective for this cyclization.

机译：通过使用0.2％mol的CuO，开发了一种通过邻位卤代烷酰基苯酮，二苯甲酮和芳基羧酸通过铜催化胺化一步合成区域选择性合成1-烷基或1-芳基-1H-吲唑的一般方法。反应涉及胺化反应，然后进行分子内脱水反应。将不同的官能化烷基芳基酮，二芳基酮和苯甲酸衍生物有效地与几种肼偶联。通常用作分子间胺化反应的催化剂的配体对此无效。环化。

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《Organic letters》 |2007年第3期|共4页
作者
Dolores Vina; Esther del Olmo; Jose L.Lopez-Perez;
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1. Regioselective Synthesis of 1-Alky I- or 1-Aryl-1H-indazoles via Copper-Catalyzed Cyclizations of 2-Haloarylcarbonylic Compounds [J] . Dolores Vina, Esther del Olmo, Jose L.Lopez-Perez Organic letters . 2007,第3期

机译：通过2-卤代芳基羰基化合物的铜催化环化反应，区域选择性合成1-烷基I-或1-芳基-1H-吲唑
2. Regioselective Synthesis of 1-Alkyl- or 1-Aryl-1H-indazoles via Copper-Catalyzed Cyclizations of 2-Haloarylcarbonylic Compounds [J] . Dolores Vina, Esther del Olmo, Jose L. Lopez-Perez, Organic letters . 2007,第3期

机译：通过2-卤代芳基羰基化合物的铜催化环化区域选择性合成1-烷基-或1-芳基-1H-吲唑
3. Regioselective synthesis of 1-alkyl- or 1-aryl-1H-indazoles via copper-catalyzed cyclizations of 2-haloarylcarbonylic compounds [J] . Vina D, del Olmo E, Lopez-Perez JL, Organic letters . 2007,第3期

机译：通过铜催化的2-卤代芳基羰基化合物的环化反应，选择性合成1-烷基或1-芳基-1H-吲唑
4. Functionalization of Organogermanium Compounds: Stereoselective Synthesis of Triols and Regioselective Synthesis of Dienes [C] . Yohei Minami, Akihito Konishi, Makoto Yasuda 日本化学会春季年会講演予稿集 . 2018

机译：有机吡喃化合物的官能化：三醇的立体选择性合成及分子区域选择性合成
5. PartI. Synthesis of N-heterocyclic furanosides and pyranosides via 5- or 6-exo-trig-radical cyclizations. Part II. (a) Palladium catalyzed silystannylative cyclization of diynes and allenynes (b) Regioselective Diels-Alder reaction of vinylsilane and its application to Papulacandin D core structure [D] . Rhee, Jong Uk 2004

机译：第一部分。通过5-或6-exo-trig-自由基环化反应合成N-杂环呋喃糖苷和吡喃糖苷。第二部分（a）钯催化的二炔和丙炔的甲硅烷基化环化反应（b）乙烯基硅烷的区域选择性Diels-Alder反应及其在Papulacandin D核结构中的应用
6. Stereoselective and Regioselective Synthesis of Heterocycles via Copper-Catalyzed Additions of Amine Derivatives and Alcohols to Alkenes [O] . Sherry R. Chemler, Shuklendu D. Karyakarte, Zainab M. Khoder -1

机译：通过铜催化胺衍生物和醇向烯烃的立体选择性和区域选择性合成杂环。
7. Regioselective Synthesis of 1-Alkyl- or 1-Aryl-1H-indazoles via Copper-Catalyzed Cyclizations of 2-Haloarylcarbonylic Compounds [O] . -1

机译：通过铜催化的2-卤芳基羰基化合物的铜催化环化来合成1-烷基 - 或1-芳基-1H-吲唑的区域选择性合成

Regioselective Synthesis of 1-Alky I- or 1-Aryl-1H-indazoles via Copper-Catalyzed Cyclizations of 2-Haloarylcarbonylic Compounds

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