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Inne
Structural analogues of selfotel.
Autorzy
Rok wydania
2016
Czasopismo
Numer woluminu
81
Strony
4947-4954
DOI
10.1021/acs.joc.6b00220
Kolekcja
Język
Angielski
Typ publikacji
Artykuł
A small library of phosphonopiperidylcarboxylic acids, analogues of NMDA antagonist selfotel (CGS 19755), was synthesized. First, the series of aromatic esters was obtained via a palladium-catalyzed cross-coupling reaction (Hirao coupling) of dialkyl phosphites with bromopyridinecarboxylates, followed by their hydrolysis. Then, hydrogenation of the resulting phosphonopyridylcarboxylic acids over PtO2 yielded the desired phosphonopiperidylcarboxylic acids. NMR studies indicated that the hydrogenation reaction proceeds predominantly by cis addition. Several compounds were obtained as monocrystal structures. Preliminary biological studies performed on cultures of neurons suggest that the obtained compounds possess promising activity toward NMDA receptors.
Adres publiczny
http://dx.doi.org/10.1021/acs.joc.6b00220
Strona internetowa wydawcy
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