Palladium(II)-catalyzed Intermolecular Cascade Cyclization of Methylenecyclopropanes with Aromatic Alkynes: Construction of Spirocyclic Compounds Containing Indene and 1,2-Dihydronaphthalene Moieties
A palladium(II)-catalyzed intermolecular cascade cyclization of methylenecyclopropanes with aromatic alkynes is reported in this paper. The reaction involves a migratory insertion of alkyne, an intramolecular Heck-type reaction, and β-H elimination, providing a series of spirocyclic compounds containing indene and 1,2-dihydronaphthalene moieties in moderate to excellent yields upon heating.
Fang, Wei,Wei, Yin,Shi, Min
(2019/05/22)
One-pot synthesis of 4-methylisoquinolines via a sequential Pd-catalyzed Heck reaction and intramolecular cyclization
An efficient, one-pot synthesis of 4-methylisoquinolines via a cascade Pd-catalyzed Heck reaction, intramolecular cyclization and isomerization has been developed. This reaction has a wide range of substrates with various functional groups, and the corresponding products have been obtained in good yields.
Synthesis of 3-aryl-2-methoxyinden-1-one (Z)-phenylhydrazones via hydrobromic acid-mediated cyclization of 2-(1-aryl-2-methoxyethenyl)benzaldehyde phenylhydrazones
2-(1-Aryl-2-methoxyethenyl)benzaldehydes 2, obtained by successive treatment of 1-(1-aryl-2-methoxyethenyl)-2-bromobenzenes 1 with BuLi and 1-formylpiperidine, were transformed to the corresponding phenylhydrazones 3 on treatment with PhNHNH2.
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
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(2008/06/13)
1-ARYL-4-SUBSTITUTED PIPERAZINES DERIVATIVES FOR USE AS CCR1 ANTAGONISTS FOR THE TREATMENT OF INFLAMMATION AND IMMUNE DISORDERS
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.