Herein, we report that binuclear copper complexes used as dehydrogenative catalysts, combined with oxygen as an oxidant and 2,2,6,6-tetramethylpiperidinyl-1-oxide (TEMPO) as an additive, are capable of effectively catalyzing the successive dehydrogenation of aromatic propanols to produce α,β-unsaturated aldehydes. This method has the advantages of high efficiency, simple operation, and oxygen as an oxidant. The reaction mechanism of continuous dehydrogenation of aromatic propanols was investigated by in situ infrared spectroscopy and control experiments. The dehydrogenation process suggested that phenylpropanol was first oxidized to arylpropanals and then underwent α,β-selective dehydrogenation of the carbonyl group to yield α,β-unsaturated aldehydes. This protocol provides insights into the design and synthesis of efficient catalysts for the preparation of α,β-unsaturated aldehydes by continuous dehydrogenation of aromatic propanols.
The solid-phase synthesis method is optimized for building chemical libraries. Furthermore, chemical libraries are essential tools in drug discovery used to identify hit compounds. We constructed a 5H-thiazolo[5',4':5,6]pyrido[2,3-b]indole derivative library using solid-phase synthesis. The indole insertion reaction at the benzylic position using a Lewis acid and the oxidative cyclization reaction using iodine were used for synthesis. Using optimized solution-phase reaction conditions, a solid-phase synthesis method comprising a total of eight steps was employed to build a 5H-thiazolo[5',4':5,6]pyrido[2,3-b]indole derivative library. In addition, we found an efficient compound library synthesis route with each synthetic step having a yield of 62-82%.
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