Conference Paper アミノアルコール有機分子触媒不斉Diels‐Alder反応を鍵反応とする新規抗インフルエンザ活性物質の合成研究
Development or new anti-influenza molecules using organocatalyzed Diels-Alder reaction of 1,2-dihydropyridines with dienophiles as a key reaction

高木, 僚平  ,  関, 千草  ,  小川, 晴子  ,  今井, 邦俊  ,  上井, 幸司  ,  中野, 博人

Tamiflu is a potent inhibitory neuraminidase that is used worldwide as a drug for influenza. However, most recently, a microbe resistant to Tamiflu was confirmed. Therefore, the development of an effective new anti-influenza molecules is needed as soon as possible. In this study, we tried to prepare a new antiviral candidate molecules having the characteristic of both Tamiflu and Relenza by using amino alcohol organocatalyzed DA reaction of 1,2-dihydropyridines with acrolein as a key reaction. We will describe that the synthesis of both the key intermediates 5 and 6 that were obtained from the chiral isoquinuclidine deriveative 3, and the preparation of new antiviral candidate molecules X, Y derived from 5, 6 and its anti-influenza activety.

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