Potent, low molecular weight renin inhibitors containing a C-terminal heterocycle: hydrogen bonding at the active site
摘要:
A series of low-nanomolar renin inhibitors containing novel C-terminal heterocycles has been designed by formally cyclizing the C-terminus of a glycol-based inhibitor to the second hydroxyl. Molecular modeling suggests that the heterocyclic oxygen hydrogen bonds as an acceptor to the flap region of renin and that the second hydroxyl in the glycol-based inhibitors behaves similarly.
Gold-Catalyzed Fluorination-Hydration: Synthesis of α-Fluorobenzofuranones from 2-Alkynylphenol Derivatives
作者:Qiang Wang、Yu Jiang、Run Sun、Xiang-Ying Tang、Min Shi
DOI:10.1002/chem.201602545
日期:2016.10.4
The AuI‐catalyzed fluorination–hydration of 2‐alkynylphenol derivatives in the presence of Selectfluor [1‐chloromethyl‐4‐fluoro‐1,4‐diazoniabicyclo‐[2.2.2]octane bis(tetrafluoroborate)] has been developed. This method provides straightforward access to α‐fluorobenzofuranones with the construction of C−O, C=O, and C−F bonds in a single step on the basis of an AuI/AuIII redox catalytic cycle. Several
在Au我催化的2- alkynylphenol衍生物的氟化水合的Selectfluor的存在[1-氯甲基-4-氟-1,4- diazoniabicyclo- [2.2.2]辛烷双(四氟硼酸盐)]已被开发。该方法可在Au I / Au III氧化还原催化循环的基础上,一步一步直接获得具有C-O,C = O和C-F键的α-氟苯并呋喃酮。还进行了一些对照实验,包括该反应的不对称变体,以深入了解反应机理。
US2409675
申请人:——
公开号:——
公开(公告)日:——
ROSENBERG, SAUL H.;DELLARIA, JOSEPH F.;KEMPF, DALE J.;HUTCHINS, CHARLES W+, J. MED. CHEM., 33,(1990) N, C. 1582-1590
作者:ROSENBERG, SAUL H.、DELLARIA, JOSEPH F.、KEMPF, DALE J.、HUTCHINS, CHARLES W+