Efficient Synthesis of Fused Triazolo[4,5-d]quinoline Derivatives via Palladium Catalysis Mediated by Tetrabutylammonium Iodide

碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所 === 100 === In Recent years, the vast number of pharmaceutical drugs and natural products that contain triazole ring system with substituents at 1, 4- position,proven to have an enhanced medicinal properties such as anti-HIV, antimicrobial, anti-inflammatory, anticonvuls...

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Bibliographic Details
Main Authors: Cheng-Hao Yang, 楊政澔
Other Authors: Jeh-Jeng Wang
Format: Others
Language:zh-TW
Published: 2012
Online Access:http://ndltd.ncl.edu.tw/handle/75051453131288225970
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Summary:碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所 === 100 === In Recent years, the vast number of pharmaceutical drugs and natural products that contain triazole ring system with substituents at 1, 4- position,proven to have an enhanced medicinal properties such as anti-HIV, antimicrobial, anti-inflammatory, anticonvulsant, anticancer and antifungal. Quinoline used in the treatment of malaria, and their antibacterial, anti-inflammatory, anti-tumours activity were proved recently. In this thesis, we report the synthesis of triazolo-quinoline/ chromene/ thiochromene via CuAAC and intramolecular electrophilic cyclization by 5 steps. And the total yield can achieve 24~38%. In order to improve the yield, we developed an efficient 3 steps methodology to synthesize our triazole derivatives with an increased total yield (45~56%), whereas earlier reported yield was about 24~38% and in 5 steps.