ARYL AND HETEROARYL-CARBOXAMIDE SUBSTITUTED HETEROARYL COMPOUNDS AS TYK2 INHIBITORS
Novel carboxamide substituted compounds of Formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Tyrosine Kinase 2 (Tyk2).
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(2021/10/15)
Nucleophilic aromatic substitution reactions under aqueous, mild conditions using polymeric additive HPMC
The use of the inexpensive, benign, and sustainable polymer, hydroxypropyl methylcellulose (HPMC), in water enables nucleophilic aromatic subsitution (SNAr) reactions between various nucleophiles and electrophiles. The mild reaction conditions facilitate a broad functional group tolerance that can be utilized for subsequent derivatization for the synthesis of pharmaceutically relevant building blocks. The use of only equimolar amounts of all reagents and water as reaction solvent reveals the greenness and sustainability of the methodology presented herein.
Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.
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(2014/04/17)
A convenient synthesis of 5-arylamino-4H-pyran-4-ones using palladium-catalyzed amination
A concise approach to 5-arylamino-4H-pyran-4-ones is described via palladium-catalyzed amination reaction. The methodology involved in this Letter is based on protection/deprotection protocols and on manipulation of the 5-hydroxy group of readily available kojic acid. It would provide a new entry to a range of 5-arylamino-4H-pyran-4-ones via Buchwald-Hartwig-type amination reaction on 4H-pyran-4-one unit.