676348-64-4Relevant articles and documents
Synthesis of 4-Quinolones: N,O-Bis(trimethylsilyl)acetamide-Mediated Cyclization with Cleavage of Aromatic C-O Bond
Pí?a, Ond?ej,Rádl, Stanislav
, p. 2336 - 2350 (2016/05/19)
The synthesis of 1,4-dihydro-4-oxoquinoline derivatives (4-quinolones) based on a BSA [N,O-bis(trimethylsilyl)acetamide]-mediated cyclization of substituted 1-(2-methoxyphenyl)-3-(alkyl/arylamino)prop-2-en-1-ones is described. The reaction belongs to a rare set of cyclizations in which a methoxy group serves as the leaving group. Reaction takes place by the action of silylating agent under mild conditions and provides high yields of pure products following simple aqueous work-up. The versatility of the approach is exemplified by a wide range of 1-alkyl/aryl 3-carboxylates and 3-nitriles that have been prepared. A crucial advantage of this approach is the facile availability of starting methoxy compounds enabling new synthetic possibilities as well as improved cost efficiency. A new approach to the synthesis of 1,4-dihydro-4-oxoquinoline (4-quinolone) derivatives using a BSA-mediated reaction was developed; this entails an example of rare cyclizations in which an OMe group serves as a leaving group. This transformation has great synthetic potential due to the phenolic framework of starting materials and the mildness of the reagent.
2-Thiopyrimidinones
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Paragraph 0260; 0261; 0262, (2013/05/22)
Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
A novel class of apical sodium-dependent bile acid transporter inhibitors: The amphiphilic 4-oxo-1-phenyl-1,4-dihydroquinoline derivatives
Kurata, Hitoshi,Suzuki, Sayaka,Ohhata, Yasuo,Ikeda, Takuya,Hasegawa, Toru,Kitayama, Ken,Inaba, Toshimori,Kono, Keita,Kohama, Takafumi
, p. 1183 - 1186 (2007/10/03)
A series of 4-oxo-1-phenyl-1,4-dihydroquinolines possessing a linker and an ammonio moiety were synthesized and found to inhibit the apical sodium-dependent bile acid transporter (ASBT). The potency of ASBT inhibition varied with the position and length o