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Article Abstract
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 5-thiazolo[5',4':5,6]pyrido[2,3-]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 5-thiazolo[5',4':5,6]pyrido[2,3-]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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