- One-pot three-component reactions of methyl ketones, phenols and a nucleophile: An expedient way to synthesize densely substituted benzofurans
-
Three-component reactions of phenylglyoxal monohydrate, phenols, and indoles were developed with the aid of acid-catalyst, which produced various densely substituted benzofurans with good to excellent yields. On the basis of this observation, a one-pot, step-wise reaction was developed by using methyl ketones instead of using phenylglyoxal component in I2/DMSO system. At last, three-component reaction offered a useful way to synthesize densely substituted benzofurans starting from simple and easily available substrates. The indole component can be replaced by some other nucleophiles, such as 1,2,4-trimethoxybenzene and thiophenol.
- Cheng, Cheng,Liu, Changhui,Gu, Yanlong
-
p. 8009 - 8017
(2015/12/31)
-
- Synthesis of 2-aroyl-(4 or 5)-aryl-1H-imidazoles and 2-hydroxy-3,6-diaryl- pyrazines via a cascade process
-
The synthesis of (4 or 5)-aryl-2-aroyl-1H-imidazoles and 2-hydroxy-3,6-diarylpyrazines from aryl methyl ketones via a cascade process of DMSO-HBr oxidation and Debus reaction was investigated. Owing to the simple starting materials, mild conditions, easy operation, high bioactivity of imidazole and pyrazine derivatives, this protocol has great potential in medicinal chemistry.
- Liu, Cong,Dai, Rong J.,Yao, Guo W.,Deng, Yu L.
-
p. 146 - 163
(2014/04/17)
-
- Design and synthesis of 2-acylbenzothiazoles via in situ cross-trapping strategy from benzothiazoles with aryl ketones
-
An I2/KOH synergistically promoted direct ring-opening aroylation of benzothiazoles with aryl ketones has been discovered. Aryl ketones were seen to act as carbonyl sources to construct 2-acylbenzothiazoles. This reaction could provide an example for the convergent integration of self-labor domino sequences based on an in situ cross-trapping strategy.
- Gao, Qinghe,Wu, Xia,Jia, Fengcheng,Liu, Meicai,Zhu, Yanping,Cai, Qun,Wu, Anxin
-
p. 2792 - 2797
(2013/04/24)
-
- Quinoxalines. Part 13: Synthesis and mass spectrometric study of aryloxymethylquinoxalines and benzo[b]furylquinoxalines
-
A series of new aryloxymethylquinoxalines, benzo[b]- and naphtho[2,1-b]furylquinoxalines, possessing potential biological activity, was prepared, characterized by IR and NMR spectroscopy and their electron ionization (EI) mass spectra studied in detail. The aryloxymethylquinoxalines were obtained by reacting halogenomethylquinoxalines with bifunctional O-nucleophiles. The benzo[b]furylquinoxalines and naphtho[2,1-b] furylquinoxalines were prepared via two routes, which differed in the order of the two cyclization steps involved in the syntheses. The composition of the ions obtained by EI mass spectrometry were determined by accurate mass measurements and the fragmentation pathways clarified by B/E linked scans and collision induced dissociation. The mass spectrometric behaviour of the compounds studied as to the possible loss of OH· radicals proved to be very characteristic.
- Starke, Ines,Sarodnick, Gerhard,Ovcharenko, Vladimir V.,Pihlaja, Kalevi,Kleinpeter, Erich
-
p. 6063 - 6078
(2007/10/03)
-
- Secondary amines and their use in pharmaceutical compositions
-
Compounds of formula (III): STR1 and esters, amides and pharmaceutically acceptable salts thereof, wherein A1 is hydrogen or methyl; A2 is hydrogen or methyl; n is 1, 2 or 3; and R is hydrogen, chlorine, bromine, hydroxy, nitro, amin
- -
-
-