- Transition-Metal-Free Decarboxylative Arylation of 2-Picolinic Acids with Arenes under Air Conditions
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A facile, transition-metal-free, and direct decarboxylative arylation of 2-picolinic acids with simple arenes is described. The oxidative decarboxylative arylation of 2-picolinic acids with arenes proceeds readily via N-chloro carbene intermediates to afford 2-arylpyridines in satisfactory to good yields under transition-metal-free conditions. This new type of decarboxylative arylation is operationally simple and scalable and exhibits high functional-group tolerance. Various synthetically useful functional groups, such as halogen atoms, methoxycarbonyl, and nitro, remain intact during the decarboxylative arylation of 2-picolinic acids.
- Zhang, Xitao,Feng, Xiujuan,Zhou, Chuancheng,Yu, Xiaoqiang,Yamamoto, Yoshinori,Bao, Ming
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supporting information
p. 7095 - 7099
(2018/11/23)
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- Palladium-catalyzed C-H alkylation of 2-phenylpyridines with alkyl iodides
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Palladium-catalyzed C-H alkylation reaction of 2-phenylpyridines with alkyl iodides has been successfully developed. The palladacycles obtained from 2-phenylpyridines should act as the key intermediates in the alkylation reaction.
- Wang, Xiaoling,Ji, Xiaoming,Shao, Changdong,Zhang, Yu,Zhang, Yanghui
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supporting information
p. 5616 - 5624
(2017/07/12)
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- A 2-substituted pyridine-based pharmaceutical intermediates the synthetic method of the compound of
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The invention relates to a synthesis method of a 2-substituted pyridine-class drug intermediate compound shown in the formula (I) (please see the formula in the specification). The method includes the steps that when catalysts, ligand, alkali and additives exist, a compound with the formula (II) and a compound with the formula (III) react in an organic solvent so that the compound shown in the formula (I) (please see the formula in the specification) can be obtained, wherein R1, R2 and R3 are independently selected from H, halogen or C-C6 alkyl groups; the formula (please see the formula in the specification) is a C6-C10 aryl group which is not substituted or has 1-2 substitutent groups or is a C4-C10 heterocyclic radical which is not substituted or has 1-2 substitutent groups, and the substitutent grous are halogen, nitro or C1-C6 alkyl groups; Hal serves as the halogen. According to the method, the catalysts, the ligand, the alkali and the additives are properly selected and combined, and therefore a high yield is achieved, and the method has good industrial prospects and good application potentiality.
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Paragraph 0045; 0046; 0047; 0048; 0049; 0050; 0051
(2016/12/22)
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- Copper-catalyzed aerobic synthesis of 2-arylpyridines from acetophenones and 1,3-diaminopropane
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A copper-catalyzed reaction providing direct access to 2-arylpyridines from acetophenones and 1,3-diaminopropane is described. A range of electronically diverse acetophenones undergo this transformation, affording 2-arylpyridines in good yields. (Chemical Equation Presented).
- Xi, Long-Yi,Zhang, Ruo-Yi,Liang, Shuai,Chen, Shan-Yong,Yu, Xiao-Qi
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supporting information
p. 5269 - 5271
(2015/01/09)
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