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
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.
Total Synthesis of Cryptophycin Analogues. Isosteric Replacement of the C−D Ester
作者:Bryan H. Norman、Thomas Hemscheidt、Richard M. Schultz、Sherri L. Andis