499146-71-3Relevant academic research and scientific papers
Sulfoximine-directed ruthenium-catalyzed ortho -C-H Alkenylation of (Hetero)Arenes: Synthesis of EP3 receptor antagonist analogue
Yadav, M. Ramu,Rit, Raja K.,Shankar, Majji,Sahoo, Akhila K.
, p. 6123 - 6134 (2014/07/21)
The reusable sulfoximine directing-group-assisted Ru(II)-catalyzed chemo- and regioselective ortho-C-H alkenylation of arenes and heteroarenes with acrylates and α,β-unsaturated ketones/vinyl sulfone is shown. The N-aroyl sulfoximine undergoes annulation with diphenylacetylene, delivering isoquinolinones and methyl phenyl sulfoxide. The present protocol is successfully employed for the synthesis of the EP3 receptor antagonist analogue.
3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 1: Discovery and exploration of the carboxyamide side chain
Asada, Masaki,Obitsu, Tetsuo,Nagase, Toshihiko,Tanaka, Motoyuki,Yamaura, Yoshiyuki,Takizawa, Hiroya,Yoshikawa, Ken,Sato, Kazutoyo,Narita, Masami,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
experimental part, p. 80 - 90 (2010/04/05)
A series of 3-(2-aminocarbonyl-4-phenoxymethylphenyl)propanoic acid analogs were synthesized and evaluated for their EP3 antagonist activity in the presence of additive serum albumin. Several compounds were biologically evaluated for their in vivo efficacy with respect to the PGE2-induced uterine contraction in pregnant rats as well as their pharmacokinetics. The discovery process of these potent and selective EP3 antagonists and their structure activity relationship are also presented.
CARBOXYLIC ACID DERIVATIVE COMPOUNDS AND DRUGS COMPRISING THESE COMPOUNDS AS THE ACTIVE INGREDIENT
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Page 184, (2010/02/07)
A carboxylic acid derivative of formula (I): wherein R1 is-COOH,-COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl,
