Nucleophilic Ring Opening of Donor–Acceptor Cyclopropanes with the Cyanate Ion: Access to Spiro[pyrrolidone-3,3′-oxindoles]
作者:Sergey V. Zaytsev、Konstantin L. Ivanov、Dmitry A. Skvortsov、Stanislav I. Bezzubov、Mikhail Ya. Melnikov、Ekaterina M. Budynina
DOI:10.1021/acs.joc.8b00922
日期:2018.8.3
The nucleophilic ringopening of donor–acceptorcyclopropanes with the cyanate ion is reported for the first time. Cyclopropanes, spiro-activated with oxindole fragments as acceptors, are shown to undergo transformations into biologically relevant spiro[pyrrolidone-3,3′-oxindoles] while being treated with potassium cyanate under microwave assistance.
Domino Michael/aza-Wittig reaction in the diastereoselective construction of spiro[azepane-4,3′-oxindoles]
作者:Konstantin L. Ivanov、Anna A. Kravtsova、Elena A. Kirillova、Mikhail Ya. Melnikov、Ekaterina M. Budynina
DOI:10.1016/j.tetlet.2019.06.037
日期:2019.7
A convenient synthetic strategy for the diastereoselective assembly of spiro[azepane-4,3′-oxindoles] was developed via a Staudinger/Michael/aza-Wittig/reduction/N-deprotection reaction sequence starting from PMB-protected oxindole-substituted ethylazides. The key step of the method is a domino self-catalytic Michael/aza-Wittig reaction wherein the phosphazene moiety acts first as the catalyst and then
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.