Stereoselective synthesis of 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as PIM kinase inhibitors inspired from marine alkaloids.
Sign Up to like & getrecommendations! Published in 2022 at "Chirality"
DOI: 10.1002/chir.23501
Abstract: We previously demonstrated that natural product-inspired 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones derivatives delivered potent and selective PIM kinases inhibitors however with non-optimal ADME/PK properties and modest oral bioavailability. Herein, we describe a structure-based scaffold decoration and a stereoselective approach… read more here.
Keywords: synthesis dihydropyrrolo; dihydropyrrolo pyrazin; pyrazin one; synthesis ... See more keywords
Multicomponent Reaction for the Synthesis of 5,6-Dihydropyrrolo[2,1-a]isoquinolines
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DOI: 10.1021/acsomega.9b03546
Abstract: A multicomponent reaction between isatin, tetrahydroisoquinoline, and terminal alkyne in the presence of benzoic acid for the synthesis of N-(substituted-2-(2-phenyl-5,6-dihydropyrrolo[2,1-a]isoquinolin-3-yl)phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamides is described. This three-component reaction proceeds via sequential formation of spirooxindole, generation of isocyanate functionality… read more here.
Keywords: reaction synthesis; multicomponent reaction; dihydropyrrolo; synthesis dihydropyrrolo ... See more keywords