Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K
摘要:
Using solid-phase synthesis, a library of novel cyclic alkoxyketones has been constructed which show strong inhibitory activity against the cysteine protease, cathepsin K (EC 3.4.22.38). (C) 2001 Published by Elsevier Science Ltd.
DOI:
10.1016/s0960-894x(00)00626-0
作为产物:
描述:
3,3-Dimethoxy-4-benzyloxycarbonylamino-tetrahydrofuran 在
钯氢气 作用下,
以
乙醇 为溶剂,
反应 12.0h,
以to afford the title compound as a yellow oil, 8 g, 100%的产率得到4,4-二甲氧基四氢-3-呋喃胺
[EN] PROTEASE INHIBITORS<br/>[FR] INHIBITEURS DE PROTEASES
申请人:SMITHKLINE BEECHAM CORPORATION
公开号:WO1998050533A1
公开(公告)日:1998-11-12
(EN) The invention relates to 3-hydroxy- and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy- or 3-keto-moiety is bonded to a tetrahydrothiophene, tetrahydrothiopyran, tetrahydrofuran or tetrahydropyran ring.(FR) Cette invention se rapporte à des composés de leucine à substitution 3-hydroxy-cyclohétéro et 3-céto-cyclohétéro, qui constituent des inhibiteurs des cystéine-protéases, en particulier la cathépsine K, et qui sont utiles dans le traitement des maladies pour lesquelles l'inhibition de la déperdition osseuse constitue un facteur. La fraction 3-hydroxy ou 3-céto est liée à un cycle tétrahydrothiophène, tétrahydrothiopyranne, tétrahydrofuranne ou tétrahydropyranne.
Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K
作者:Ashley E. Fenwick、Bénédicte Garnier、Andrew D. Gribble、Robert J. Ife、Anthony D. Rawlings、Jason Witherington
DOI:10.1016/s0960-894x(00)00626-0
日期:2001.1
Using solid-phase synthesis, a library of novel cyclic alkoxyketones has been constructed which show strong inhibitory activity against the cysteine protease, cathepsin K (EC 3.4.22.38). (C) 2001 Published by Elsevier Science Ltd.