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    6-alkylamino-2,2′-disubstituted-7,8-disubstituted-2H-1-benzopyran derivatives as 5-lipoxygenase inhibitor
    2.
    发明授权
    6-alkylamino-2,2′-disubstituted-7,8-disubstituted-2H-1-benzopyran derivatives as 5-lipoxygenase inhibitor 失效

    公开(公告)号：US07368575B2

    公开(公告)日：2008-05-06

    申请号：US10970046

    申请日：2004-10-20

    申请人： Young-Dae Gong ,  Hyae-Gyeong Cheon ,  Young-Sik Cho ,  Jin-Soo Seo ,  Jong-Yeon Hwang ,  Ji-Yeon Park ,  Sung-Eun Yoo

    发明人： Young-Dae Gong ,  Hyae-Gyeong Cheon ,  Young-Sik Cho ,  Jin-Soo Seo ,  Jong-Yeon Hwang ,  Ji-Yeon Park ,  Sung-Eun Yoo

    IPC分类号： C07D311/00 ,  C07D405/00

    CPC分类号： C07D311/70 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12

    摘要： When a multi-step process reaction is carried out in a solution, it generally requires several treatments and purification procedures to go through with after the reaction, however, the inventive method for preparing 2,2′-disubstituted-3,4-dihydro-7,8-disubstituted-6-amino benzopyran derivative using a solid-phased synthetic method simplifies the treatment and purification procedures after the reaction, which makes possible to efficiently construct numerous drug-like libraries. In particular, since the inventive method of the present invention comprises the steps of introducing a carbonate linker of formula 2 into Wang resin used as a common solid support (Step 1); synthesizing various benzopyran in a carbamate form of formula 3 as a key intermediate by reacting various amino benzopyran derivatives with the carbamate resin of formula 2 (Step 2); synthesizing 2,2′-disubstituted-3,4-2H-6-substituted benzopyran resin of formula 4 (Step 3); and synthesizing 2,2′-disubstituted-3,4-2H-6-alkylamino benzopyran derivative of formula 1 using a dichloromethane solution containing TFA or an organic solvent containing an organic acid, the inventive method is capable of efficiently synthesizing various 2,2′-disubstituted-3,4-2H-6-alkylamino benzopyran derivatives.Consequently, the present invention has developed a new technique for constructing 2,2′-disubstituted-3,4-2H-6-alkylamino benzopyran library using a solid-phase parallel synthetic method and makes increased the applicability of combinatorial chemical synthetic method. Further, 2,2′-disubstituted-3,4-2H-6-alkylamino benzopyran derivative prepared by the inventive method has a high inhibitory effect to 5-lipoxygenase (5-LO) activity, and therefore, can be effectively used for developing a new propylactic or therapeutic drug for leukotriene activation-related diseases such as chronic inflammation, rheumatic arthritis, colitis, asthma and psoriasis.