Palladium-Catalyzed Acylation Reactions: A One-Pot Diversified Synthesis of Phthalazines, Phthalazinones and Benzoxazinones
A sequential one-pot strategy for the diversified synthesis of phthalazines, phthalazinones and benzoxazinones was presented. This strategy proceeds through [Pd]-catalyzed acylation and nucleophilic cyclocondensation with dinucleophilic reagents. This process was based on direct coupling with simple bench-top aldehydes without the assistance of directing group and without activating the carbonyl group. The process is highly advantageous because it employs simple nitrogen-based nucleophiles, and non-toxic and readily accessible aldehydes as the carbonyl source. Most importantly, the strategy was applied to the one-pot synthesis of PDE-4 inhibitor.
Suchand, Basuli,Satyanarayana, Gedu
p. 2233 - 2246
(2018/06/04)
Iodine-promoted oxidative conversion of o-vinyl diaryl ketones into o-acetyl diaryl ketones, synthesis of 1-methyl-4-arylphthalazines as analogues of podophyllotoxin
A new method is described for the metal-free oxidation of o-vinyl diaryl ketones in the presence of molecular iodine or N-iodosuccinimide to give o-acetyl diaryl ketones. This transformation involves the initial formation of an iodohydrin, and the o-carbo
Iodine-promoted oxidative conversion of o-vinyl diaryl ketones into o-acetyl diaryl ketones, synthesis of 1-methyl-4-arylphthalazines as analogues of podophyllotoxin
A new method is described for the metal-free oxidation of o-vinyl diaryl ketones in the presence of molecular iodine or N-iodosuccinimide to give o-acetyl diaryl ketones. This transformation involves the initial formation of an iodohydrin, and the o-carbo