64714-85-8Relevant academic research and scientific papers
Synthesis of the Sex Pheromone of the Oleander Scale (Aspidiotus nerii)
Casta?eda, Mary Monta?o,Bargues, Javier Marzo,Primo, Jaime,Fuertes, Ismael Navarro
, p. 8578 - 8588 (2019/09/04)
A total synthesis of the oleander scale [Aspidiotus nerii (Bouche)] sex pheromone, the unique sesquiterpenoid containing a cyclobutane moiety of this class of compounds, has been developed. In order to implement this sex pheromone as a new environmentally
Optimization of P2Y12 Antagonist Ethyl 6-(4-((Benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate (AZD1283) Led to the Discovery of an Oral Antiplatelet Agent with Improved Druglike Properties
Kong, Deyu,Xue, Tao,Guo, Bin,Cheng, Jianjun,Liu, Shunyin,Wei, Jianhai,Lu, Zhengyu,Liu, Haoran,Gong, Guoqing,Lan, Tian,Hu, Wenhao,Yang, Yushe
supporting information, p. 3088 - 3106 (2019/04/01)
P2Y12 antagonists are widely used as antiplatelet agents for the prevention and treatment of arterial thrombosis. Based on the scaffold of a known P2Y12 antagonist AZD1283, a series of novel bicyclic pyridine derivatives were designed and synthesized. The cyclization of the ester substituent on the pyridine ring to the ortho-methyl group led to lactone analogues of AZD1283 that showed significantly enhanced metabolic stability in subsequent structure-pharmacokinetic relationship studies. The metabolic stability was further enhanced by adding a 4-methyl substituent to the piperidinyl moiety. Compound 58l displayed potent inhibition of platelet aggregation in vitro as well as antithrombotic efficacy in a rat ferric chloride model. Moreover, 58l showed a safety profile that was superior to what was observed for clopidogrel in a rat tail-bleeding model. These results support the further evaluation of compound 58l as a promising drug candidate.
6-(2-Haloethyl)-2,2-dimethyl-4H-1,3-dioxins: versatile haloethyl vinyl ketone equivalents for carbocycle construction
Greshock, Thomas J.,Funk, Raymond L.
, p. 5437 - 5439 (2007/10/03)
6-(2-Iodoethyl)-2,2-dimethyl-4H-1,3-dioxin has been prepared in five steps from ethyl acetoacetate. A variety of enolates were then alkylated with this iodide. The resulting 6-alkyl-4H-1,3-dioxins were either subjected to further transformations and/or he
Synthesis of δ-hydroxy-β-oxo esters using sonochemical Blaise reaction
Narkunan, Kesavaram,Uang, Biing-Jiun
, p. 1713 - 1714 (2007/10/03)
A simple and convenient synthesis of δ-hydroxy-β-oxo esters starting from β-hydroxynitriles and ethyl bromoacetate using zinc under sonication is reported.
Condensation of Diethyl Acetonedicarboxylate. IV. Regioselective Reaction of Diethyl Acetonedicarboxylate-magnesium Complex
Yamato, Masatoshi,Kusunoki, Youichiro
, p. 2832 - 2836 (2007/10/02)
The reactivity of diethyl acetonedicarboxylate (DADC)-magnesium complex (1a, b) was examined.The Michael reaction of 1a, b gave the regioselectively monoalkylated derivative (2 or 3) of DADC.Reaction of 1a with nucleophilic reagents, LiAlH4 or alkylamines
