77770-09-3Relevant articles and documents
EP2 ANTAGONIST
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, (2022/05/05)
A drug is provided, which containing, as an active ingredient, a compound having an antagonistic activity against an EP2 receptor in the prevention and/or treatment of a disease associated with the activation of an EP2 receptor. A compound represented by general formula (I-A): (wherein all symbols have the same meanings as those described in the specification) or a pharmaceutically acceptable salt thereof is useful as a pharmaceutical ingredient having a potent antagonistic activity against an EP2 receptor in the prevention and/or treatment of a disease associated with the activation of an EP2 receptor.
Negishi cross-coupling reaction as a route to isocombretastatins
Malysheva, Yulia B.,Buchvalova, Svetlana Y.,Svirshchevskaya, Elena V.,Fokin, Valery V.,Fedorov, Alexey Y.
, p. 1772 - 1776 (2013/09/12)
A series of isocombretastatins A has been synthesized by a new method based on the Negishi cross-coupling reaction in 19-84% yields. Five of the synthesized compounds exhibit high cytotoxic activity in nanomolar concentrations (IC50 = 1-100 n) towards Jurkat, K562, Colo357, and A549 cell lines. Georg Thieme Verlag Stuttgart · New York.
Electrochemical C-H amination: Synthesis of aromatic primary amines via N -arylpyridinium ions
Morofuji, Tatsuya,Shimizu, Akihiro,Yoshida, Jun-Ichi
supporting information, p. 5000 - 5003 (2013/05/22)
We have developed a new method for C-H amination of aromatic compounds based on electrochemical oxidation of aromatic compounds in the presence of pyridine followed by the reaction of the resulting N-arylpyridinium ions with an alkylamine. This new transformation serves as a powerful method for synthesizing aromatic primary amines from aromatic compounds without using metal catalysts and harsh chemical reagents. High chemoselectivity of the present method is demonstrated by C-H amination of aromatic compounds bearing a nitro group to give a key intermediate for the synthesis of VLA-4 antagonist.