Palladium Catalyzed Cross-Coupling Of 3-Methylthiophene-2-Carbonyl Chloride With Aryl/Het-Aryl Boronic Acids: A Convenient Method For Synthesis Of Thienyl Ketones

ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY(2017)

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摘要
Bi-aryl ketones are important motifs in large number of pharmaceutical compounds and natural products. A protocol for the synthesis of thienyl ketones has been developed via Pd (0) catalyzed cross-coupling reaction. The desired thienyl ketones (3a-x) were synthesized by cross coupling of 3-methylthiophene-2-carbonyl chloride with variety of aryl/heteroaryl-boronic acids in good to excellent yields (46-91%) under mild conditions (1.5 eq Cs2CO3 at 50 degrees C). Different functional groups were well tolerated under the developed reaction conditions.
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关键词
Coupling, synthesis, palladium, arylboronic acid, thienyl ketone
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