72420-37-2Relevant academic research and scientific papers
Electroreductive acylation of aromatic ketones with acylimidazoles
Kise, Naoki,Agui, Syun,Morimoto, Shinji,Ueda, Nasuo
, p. 9407 - 9410 (2007/10/03)
The intermolecular reductive coupling of aromatic ketones with acylimidazoles was effected by electroreduction in the presence of chlorotrimethylsilane and gave α-trimethylsiloxy ketones and esters. The best result was obtained using Bu4NPF6 as a supporting electrolyte and a Pb cathode in THF. The α-trimethylsiloxy-containing products were transformed to the corresponding α-hydroxy ketones and esters by treatment with TBAF in THF. This method was also effective for the intramolecular reductive coupling of δ- and ε-keto acylimidazoles.
Analogues of oxybutynin. Synthesis and antimuscarinic and bladder activity of some substituted 7-amino-1-hydroxy-5-heptyn-2-ones and related compounds
Carter,Noronha-Blob,Audia,Dupont,McPherson,Natalie Jr.,Rzeszotarski,Spagnuolo,Waid,Kaiser
, p. 3065 - 3074 (2007/10/02)
Oxybutynin chloride [4-(diethylamino)-2-butynyl α-cyclohexyl-α-hydroxybenzeneacetate hydrochloride, Ditropan] is widely used for the relief of symptoms in neurogenic bladder. This is a result of its combined anticholinergic, antispasmodic, and local anesthetic activities. In a study directed toward development of agents possessing the beneficial properties of oxybutynin, but having a longer duration of action, a series of metabolically more stable keto analogues of the parent ester, i.e. substituted 7-amino-1-hydroxy-5-heptyn-2-ones along with some analogues and derivatives, was prepared and evaluated for in vitro and in vivo antimuscarinic action in guinea pig preparations. Several members of the series were potent antimuscarinics having a longer duration of activity than that of oxybutynin in a guinea pig cystometrogram model. On the basis of its in vitro and in vivo antimuscarinic activity, coupled with a 5-fold greater duration of action than that of oxybutynin, 1-cyclobutyl-7-(dimethylamino)-1-hydroxy-1-phenyl-5-heptyn-2-one (14b) was selected for clinical evaluation.
Hypolipidemic 4,5-Dihydro-4-oxo-5,5-disubstituted-2-furancarboxylic Acids
Jirkovski, Ivo,Cayen, Mitchell, N.
, p. 1154 - 1156 (2007/10/02)
A series of novel 4,5-dihydro-4-oxo-5,5-disubstituted-2-furancarboxylic acids was synthesized and shown to possess potent hypotriglyceridemic activity in normal rats.In contrast to clofibrate, none of the present compounds altered liver weight at any dose
Hypolipidemic derivatives of 4,5-dihydro-4-oxofuran-2-carboxylic acid
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, (2008/06/13)
Derivatives of 4,5-dihydro-4-oxofuran-2-carboxylic acid characterized by having two substituents at position 5 and in addition being optionally further substituted at position 3 with a lower alkyl group, as well as esters therefor are disclosed. The foreg
Process for preparing 4,5-dihydro-4-oxofuran-2-carboxylic acid derivatives
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, (2008/06/13)
Derivatives of 4,5-dihydro-4-oxofuran-2-carboxylic acid characterized by having two substituents at position 5 and in addition being optionally further substituted at position 3 with a lower alkyl group, as well as esters therefor are disclosed. The foreg
