Synthesis of N-Alkyl-Substituted 4-Quinolones via Tandem Alkenyl and Aryl C-N Bond Formation
摘要:
N-Alkyl-substituted 4-quinolones are present as the key structural motif in many marketed drugs. An efficient one-step tandem amination approach was developed to afford N-alkyl-substituted 4-quinolones in high yields from easily accessible o-chloroaryl acetylenic ketones and functionalized alkyl amines. The approach complements and extends our previous work. Compared with other reported methods, the current method provides a very simple and convenient route.
Lewis and Brønsted Acid Cocatalyzed Reductive Deoxyallenylation of Propargylic Alcohols with 2-Nitrobenzenesulfonylhydrazide
作者:Zhaohong Liu、Peiqiu Liao、Xihe Bi
DOI:10.1002/chem.201404692
日期:2014.12.22
Reductivedeoxyallenylation of sterically hindered tertiary propargylicalcohols was realized on reaction with 2‐nitrobenzenesulfonylhydrazide (NBSH) by the combined use of Lewis and Brønstedacid catalysts. This method features a broad substrate scope, mild reaction conditions, and good functional‐group tolerance, and affords various mono‐, di‐, and trisubstituted allenes in good‐to‐excellent yields