- BENZOXAZINONE DERIVATIVE
-
[PROBLEMS] To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases. [MEANS FOR SOLVING PROBLEMS] The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents -O-, -NH-, etc.; and Y1, Y2, Y3, and Y4 each independently represents -CH-, -N-, etc.].
- -
-
Page/Page column 32
(2010/08/07)
-
- Discovery of novel benzoxazinones as potent and orally active long chain fatty acid elongase 6 inhibitors
-
A series of benzoxazinones was synthesized and evaluated as novel long chain fatty acid elongase 6 (ELOVL6) inhibitors. Exploration of the SAR of the UHTS lead 1a led to the identification of (S)-1y that possesses a unique chiral quarternary center and a
- Mizutani, Takashi,Ishikawa, Shiho,Nagase, Tsuyoshi,Takahashi, Hidekazu,Fujimura, Takashi,Sasaki, Takahide,Nagumo, Akira,Shimamura, Ken,Miyamoto, Yasuhisa,Kitazawa, Hidefumi,Kanesaka, Maki,Yoshimoto, Ryo,Aragane, Katsumi,Tokita, Shigeru,Sato, Nagaaki
-
supporting information; experimental part
p. 7289 - 7300
(2010/06/16)
-
- Synthesis of a New Generation Reverse Transcriptase Inhibitor via the BCl3/GaCl3-induced Condensation of Anilines with Nitriles (Sugasawa Reaction)
-
The synthesis of 1 was achieved in high overall yield through a mechanism-based improvement of the preparation of o-acyl anilines.
- Houpis, Ioannis N.,Molina, Audrey,Douglas, Alan W.,Xavier, Lyndon,Lynch, Joseph,et al.
-
p. 6811 - 6814
(2007/10/02)
-
- In situ NMR spectroscopic studies of aniline ortho acylation ("sugasawa reaction"): The nature of reaction intermediates and Lewis acid influence on yield
-
Ortho acylation of anilines by nitriles in the presence of BCl3 and a second Lewis acid appear to proceed through an intermediate "supercomplex" including all four components. Yield improvements were obtained based on recognition that chloride affinity of the second Lewis acid governs supercomplex formation. Aniline protonation was found to be the cause of incomplete reaction.
- Douglas,Abramson,Houpis,Karady,Molina,Xavier,Yasuda
-
p. 6807 - 6810
(2007/10/02)
-