亚甲基缩醛与三甲基甲硅烷基三氟甲磺酸酯-2,2'-联吡啶联合进行轻度脱保护。
Mild deprotection of methylene acetals in combination with trimethylsilyl triflate-2,2'-bipyridyl.
作者信息
Fujioka Hiromichi, Senami Kento, Kubo Ozora, Yahata Kenzo, Minamitsuji Yutaka, Maegawa Tomohiro
机构信息
Graduate School of Pharmaceutical Sciences, Osaka University, Osaka 565-0871, Japan.
出版信息
Chem Pharm Bull (Tokyo). 2010 Mar;58(3):426-8. doi: 10.1248/cpb.58.426.
The facile deprotection of methylene acetal protection of diols under mild conditions is established. The combination of trimethylsilyl triflate (TMSOTf) and 2,2'-bipyridyl followed by a weakly acidic hydrolysis was effective and the substrates having acid sensitive functional groups can be tolerated under the stated conditions. The selective deprotection between methylene acetal and benzophenone ketal was achieved.
已确立在温和条件下对二醇的亚甲基缩醛保护进行简便脱保护的方法。三氟甲磺酸三甲基硅酯（TMSOTf）与2,2'-联吡啶组合，随后进行弱酸性水解是有效的，并且在所述条件下具有酸敏感官能团的底物可以耐受。实现了亚甲基缩醛和二苯甲酮缩酮之间的选择性脱保护。
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