COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
申请人:CHIESI FARMACEUTICI S.p.A
公开号:US20140161736A1
公开(公告)日:2014-06-12
Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
Natural kaolinitic clay possessing transition metals such as Fe and Ti in its lattice has been found to catalyze efficiently the chemoselectiveacetalization and thioacetalization of variety of carbonyl compounds with ethane-1,2-diol and ethane-1,2-dithiolrespectively.
1,3-Disubstituted tetrabutyldistannoxanes catalyze acetilization of carbonyl compounds undermildconditions. Thorough investigations of factors influencing this reaction are given. A variety of synthetically useful carbonyl compounds are efficiently converted to acetals. In particular, acetilization of cyclic α,β-unsaturated ketones is readily achieved which have met with only limited success so far
Carbonyl compounds 1 were converted to the corresponding 1,3-dioxolanes 2 and 1,3-dioxanes 4 with ethylene glycol and 2,2-dimethyl-1,3-propandiol, respectively, in the presence of 1-3 mol% of N-(benzyl, 4-methylbenzyl or 4-methoxybenzyl)-2(or -4)-cyanopyridinium hexafluoroantimonates 3. The catalyst 3d was also effective for the tetrahydropyranylation.