作者:Xiao-Shan Ning、Xin Liang、Kang-Fei Hu、Chuan-Zhi Yao、Jian-Ping Qu、Yan-Biao Kang
DOI:10.1002/adsc.201701512
日期:2018.4.17
A Pd‐tBuONO co‐catalyzed scalable and practical synthesis of indoles with molecular oxygen as terminal oxidant is developed. Either terminal or internal 2‐vinylanilines could be smoothly converted to desired indoles under one general condition. This method has been evaluated in the large scale synthesis of indomethacin and a potential anti‐breast cancer drug candidate 1.
Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R2 is -OH or -OP(O)(OH)2; and R1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Enantioselective Synthesis of Functionalized Arenes by Nickel‐Catalyzed Site‐Selective Hydroarylation of 1,3‐Dienes with Aryl Boronates
作者:Justin S. Marcum、Tiffany R. Taylor、Simon J. Meek
DOI:10.1002/anie.202004982
日期:2020.8.10
A catalytic method for the site‐selective and enantioselective synthesis of functionalized arenes by the intermolecular hydroarylation of terminal and internal 1,3‐dienes with aryl pinacolato boronates is reported. The reactions are promoted by 5.0 mol % of a readily available monodentate phosphoramidite‐Ni complex in ethanol, affording a variety of enantioenriched products in up to 96 % yield and
NiH-Catalyzed Reductive Relay Hydroalkylation: A Strategy for the Remote C(sp<sup>3</sup>
)−H Alkylation of Alkenes
作者:Fang Zhou、Jin Zhu、Yao Zhang、Shaolin Zhu
DOI:10.1002/anie.201712731
日期:2018.4.3
The terminal‐selective, remoteC(sp3)−H alkylation of alkenes was achieved by a relay process combining NiH‐catalyzed hydrometalation, chain walking, and alkylation. This method enables the construction of unfunctionalized C(sp3)−C(sp3) bonds under mild conditions from two simple feedstock chemicals, namely olefins and alkyl halides. The practical value of this transformation is further demonstrated