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Enantioselective Synthesis of the Unsaturated Fragment of Callyspongiolide

A synthesis of the unsaturated side chain of callyspongiolide has been accomplished from two chiral building blocks prepared by catalytic asymmetric procedures applied on simple starting materials. The synthesis of the chiral benzylic alcohol was based on an enantioselective aldol reaction of a substituted benzaldehyde catalyzed by a chiral amine, whereas the chiral homoallyl alcohol was prepared by the enantioselective crotylboration of iodomethacryl aldehyde catalyzed by a chiral phosphoric acid. Both fragments were joined together by using standard Sonogashira coupling conditions.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

Extracurricular laboratory:new discovery of 51207-66-0

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Substituted phenyl compounds with immunosuppressing activity and pharmaceutical compositions

The invention provides substituted phenyl compounds of general formula STR1wherein R 1, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Ureas with histamine H3-antagonist receptor activity-A new scaffold discovered by lead-hopping from cinnamic acid amides

A group of tri and tetrasubstituted urea derivatives have been found to be hH3-antagonists. The most potent compounds were found in the class of (piperazine-1-yl)-(piperidine-1-yl)-methanones which in addition showed negligible hERG inhibition.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES

The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI