公开(公告)号：US20110028738A1

公开(公告)日：2011-02-03

申请号：US12921597

申请日：2009-01-08

申请人： Kiyomi Kakiuchi ,  Ken Tsutsumi ,  Satoru Kitani ,  Kazuki Sugawara ,  Yoshinori Gosyo

发明人： Kiyomi Kakiuchi ,  Ken Tsutsumi ,  Satoru Kitani ,  Kazuki Sugawara ,  Yoshinori Gosyo

IPC分类号： C07D335/06

CPC分类号： C07F9/655372 ,  C07D335/06 ,  C07D409/04 ,  C07H13/12 ,  C07J33/00 ,  Y02P20/55

摘要： The present invention provides a photolabile protecting group that can be removed by light irradiation under mild conditions. More specifically, the present invention provides a method comprising protecting a reactive functional group (e.g., a hydroxyl group, amino group, carboxyl group, carbonyl group, phosphodiester group, etc.) by the photolabile protecting group, and then removing the photolabile protecting group simply by light irradiation under neutral conditions.The present invention relates to a compound represented by Formula (3): wherein Ar1 is an optionally substituted aromatic or heteroaromatic ring, Ar2 is an optionally substituted aryl or heteroaryl group, X is a leaving group, and n is an integer of 1 or 2; and a method of protecting and deprotecting an amino group etc. using the compound.

摘要翻译： 本发明提供可以在温和条件下通过光照射除去的光不稳定保护基。 更具体地说，本发明提供了通过光不稳定保护基保护反应性官能团（例如羟基，氨基，羧基，羰基，磷酸二酯基等），然后除去光不稳定保护基 简单地在中性条件下通过光照射。 本发明涉及由式（3）表示的化合物：其中Ar 1是任选取代的芳族或杂芳族环，Ar 2是任选取代的芳基或杂芳基，X是离去基团，n是1或2的整数 ; 以及使用该化合物保护和脱保护氨基等的方法。