Partial and full agonists of A1 adenosine receptors
申请人:Zablocki Jeff
公开号:US20060135467A1
公开(公告)日:2006-06-22
Disclosed are novel compounds that are partial and full A
1
adenosine receptor agonists, useful for treating various disease states, in particular the supraventricular tachycardias, emesis, angina, myocardial infarction and hyperlipidemia.
Herein we report Lewis acid HfCl4-catalyzed [4 + 2] cycloaddition between β,γ-unsaturated α-keto esters and various symmetric or unsymmetric alkynes, giving the desired polysubstituted 4H-pyrans in up to 98% yield and with excellent regioselectivity (>99:1) via a vinyl carbocation under mild conditions.