Benzylic C–H arylation of azaarylmethanes with aryl sulfides has been developed by using a Pd-NHC catalyst and an amide base. Various azaarylmethanes and aryl sulfides were involved in the reaction to afford the corresponding diarylmethanes in good to excellent yields. Moreover, triarylmethane synthesis was accomplished through iterative arylations of 2- or 4-methylpyridine with two different aryl
highly efficient and practical method for incorporation of the arylmethylpyridyl moiety into diverse molecules has been developed. This method features the transition metal-free light-induced room temperature transformation of pyridotriazoles into pyridyl carbenes, which are capable of smooth arylation, X–H insertion, and cyclopropanation reactions. The synthetic usefulness of the developed method was
Rh(I)-catalyzed asymmetric approach for the intermolecular functionalization of C(sp3)–H bonds is reported. For the first time, unsymmetrical N-heterocyclic carbenes (NHCs) were used for asymmetric catalysis that is capable of achieving not only high site-selectivity but also enantioselectivity. The Rh(I)/NHC* catalytic systems were applied to asymmetric directC(sp3)–Harylation, which provides a synthetic
BISACODYL AND ITS ANALOGUES AS DRUGS FOR USE IN THE TREATMENT OF CANCER
申请人:Feve Marie
公开号:US20140186872A1
公开(公告)日:2014-07-03
The present invention provides compounds having the formula A: (A) or pharmaceutically acceptable salt thereof, wherein W, R1, R2 and R5 are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as cytotoxic agents towards proliferating and/or quiescent cancer stem cells, and thus are useful, for example, for the treatment of cancer.
Iron-Catalyzed C-H Bond Functionalization for the Exclusive Synthesis of Pyrido[1,2-<i>a</i>]indoles or Triarylmethanols
作者:Iyyanar Karthikeyan、Govindasamy Sekar
DOI:10.1002/ejoc.201403233
日期:2014.12
The efficient and selective iron-catalyzed C–H activation of 2-benzhydrylpyridine derivatives was employed for the preparation of pyrido[1,2-a]indoles through an intramolecular C–H amination reaction. In the presence of molecularoxygen as the sole oxidant, the same 2-benzhydrylpyridines were also used for the synthesis of the corresponding tertiary alcohols. In these approaches, the iron catalyst