A general method for copper-catalyzed deprotonative dimerization of arenes by employing oxygen as the terminal oxidant has been developed. Electron-rich and electron-poor heterocycles as well as electron-poor arenes are reactive. The method is tolerant to functionalities such as nitro, cyano, dialkylamino, and ester groups.
A general method for copper-catalyzed deprotonative dimerization of arenes by employing oxygen as the terminal oxidant has been developed. Electron-rich and electron-poor heterocycles as well as electron-poor arenes are reactive. The method is tolerant to functionalities such as nitro, cyano, dialkylamino, and ester groups.
C5A RECEPTOR MODULATORS
申请人:IDORSIA PHARMACEUTICALS LTD
公开号:US20200347029A1
公开(公告)日:2020-11-05
The present invention relates to derivatives of formula (I)
wherein ring A, X, Y, Z, R
1
, R
2
, R
3
and R
4
are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as C5a receptor modulators.
Nickel, Manganese, Cobalt, and Iron-Catalyzed Deprotonative Arene Dimerization
A number of first-row transition metal salts catalyze deprotonative dimerization of acidic arenes. Under the atmosphere of oxygen, nickel, manganese, cobalt, and Iron chlorides have been shown to dimerize five- and six-membered ring heterocycles as well as electron-poor arenes. Both tetramethylpiperidide and dicyclohexylamide bases can be employed; however, the former afford slightly higher yields.