5632-14-4Relevant articles and documents
Method for synthesizing substituted quinoline derivative 4- through palladium catalysis (by machine translation)
-
Paragraph 0032-0034, (2020/01/08)
The invention belongs to the technical field of 4 - synthetic chemistry, and particularly. relates to a method for synthesizing a substituted quinoline derivative with palladium through palladium catalysis, Cs. 2 CO3 The method disclosed by, the 60-80 °C invention is 5-8 simple, and green, in 4 - synthetic process,has excellent selectivity and high yield, and has a wide substrate range, and the method has a wide, application value in the fields of pharmaceutical chemistry, biochemistry and the like. (by machine translation)
One-pot borylation/Suzuki-Miyaura sp2-sp3 cross-coupling
Whitaker, Luke,Harb, Hassan Y.,Pulis, Alexander P.
, p. 9364 - 9367 (2017/08/23)
We describe the first one-pot borylation/Suzuki-Miyaura sp2-sp3 cross-coupling between readily available aryl (pseudo)halides and activated alkyl chlorides. This method streamlines the synthesis of diaryl methanes, α-aryl carbonyls and allyl aryl compounds, substructures that are commonly found in life changing drug molecules.
Base metal-catalyzed benzylic oxidation of (aryl)(heteroaryl)methanes with molecular oxygen
Sterckx, Hans,De Houwer, Johan,Mensch, Carl,Herrebout, Wouter,Tehrani, Kourosch Abbaspour,Maes, Bert U.W.
supporting information, p. 144 - 153 (2016/04/05)
The methylene group of various substituted 2- and 4-benzylpyridines, benzyldiazines and benzyl(iso)quinolines was successfully oxidized to the corresponding benzylic ketones using a copper or iron catalyst and molecular oxygen as the stoichiometric oxidant. Application of the protocol in API synthesis is exemplified by the alternative synthesis of a precursor to the antimalarial drug Mefloquine. The oxidation method can also be used to prepare metabolites of APIs which is illustrated for the natural product papaverine. ICP-MS analysis of the purified reaction products revealed that the base metal impurity was well below the regulatory limit.