Access to functionalized thienopyridines via a reagent-capsule-assisted coupling, thiolation and cyclization cascade sequence

作者：Cai, Jialing; Huang, Shuo; He, Ruenfa; Chen, Lu; Chen, Donghan; Jiang, Shaohua; Li, Bin^*; Li, Yibiao^*

来源：Organic and Biomolecular Chemistry, 2017, 15(2): 333-337.

DOI：10.1039/c6ob02351g

• ONE-POT SYNTHESIS
• DERIVATIVES
• INHIBITORS
• DISCOVERY
• KINASE
• IDENTIFICATION
• PARAFFIN
• CATALYST
• DISCONTINUATION
• HETEROCYCLES

Thienopyridines and related heterocycles were prepared in a straightforward manner in moderate to good yields and under mild conditions by palladium-catalysed cross-coupling of ortho-fluorinated iodopyridines and terminal alkynes, followed by a reagent-capsule-assisted thiolation cyclization process. By applying paraffin wax capsules to prevent catalyst poisoning and undesired side reactions, the separation and purification processes were reduced.

• 出版日期2017-1-14
• 单位五邑大学