Nickel-Catalyzed Enantioselective α-Alkenylation of <i>N</i>-Sulfonyl Amines: Modular Access to Chiral α-Branched Amines
作者:Lun Li、Yu-Cheng Liu、Hang Shi
DOI:10.1021/jacs.1c00622
日期:2021.3.24
α-branched amines are common structural motifs in functional materials, pharmaceuticals, and chiral catalysts. Therefore, developing efficient methods for preparing compounds with these privileged scaffolds is an important endeavor in synthetic chemistry. Herein, we describe an atom-economical, modular method for a nickel-catalyzed enantioselective α-alkenylation of readily available linear N-sulfonyl amines
PYRIMIDOOXAZOCINE DERIVATIVES AS MTOR - INHIBITORS
申请人:SANOFI
公开号:US20140378433A1
公开(公告)日:2014-12-25
The invention relates to bicydic heterocyclic derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.
本发明涉及一般式(I)的双环杂环衍生物,以及制备它们的过程和它们的治疗用途。
Pyrimidooxazocine derivatives as mTOR-inhibitors
申请人:SANOFI
公开号:US09120812B2
公开(公告)日:2015-09-01
The invention relates to bicyclic heterocyclic derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.
本发明涉及一般式(I)的双环杂环衍生物,其制备过程及其治疗用途。
Structure-Based Design of Novel, Urea-Containing FKBP12 Inhibitors
作者:Peter S. Dragovich、John E. Barker、Judy French、Michael Imbacuan、Vincent J. Kalish、Charles R. Kissinger、Daniel R. Knighton、Cristina T. Lewis、Ellen W. Moomaw、Hans E. Parge、Laura A. K. Pelletier、Thomas J. Prins、Richard E. Showalter、John H. Tatlock、Kathleen D. Tucker、J. Ernest Villafranca
DOI:10.1021/jm950798a
日期:1996.1.1
The structure-based design and subsequent chemical synthesis of novel, urea-containing FKBP12 inhibitors are described. These compounds are shown to disrupt the cis-trans peptidylprolyl isomerase activity of FKBP12 with inhibition constants (K-i,K-app) approaching 0.10 mu M. Analyses of several X-ray crystal structures of FKBP12-urea complexes demonstrate that the urea-containing inhibitors associate with FKBP12 in a manner that is similar to, but significantly different from, that observed for the natural product FK506.
[EN] PYRIMIDOOXAZOCINE DERIVATIVES AS MTOR - INHIBITORS<br/>[FR] DÉRIVÉS DE PYRIMIDOOXAZOCINE UTILES COMME INHIBITEURS DE mTOR
申请人:SANOFI SA
公开号:WO2013111106A1
公开(公告)日:2013-08-01
The invention relates to bicydic heterocyclic derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.