Open AccessNovel Solution- and Solid-Phase Syntheses of Heterocyclic Systems
Author(s) -
Gaelle Cabon,
Bérangère Gaucher,
Aline Gégout,
Sophie Heulle,
Thierry Masquelin
Publication year - 2003
Publication title -
chimia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.387
H-Index - 55
eISSN - 2673-2424
pISSN - 0009-4293
DOI - 10.2533/000942903777679280
Subject(s) - combinatorial chemistry , solid phase synthesis , context (archaeology) , chemistry , bicyclic molecule , phase (matter) , stereochemistry , organic chemistry , biology , biochemistry , peptide , paleontology
Heterocyclic compounds are an attractive source of screening library structures because they possess varied structural diversity and can exhibit potent biological activity. In this context, we present some of our new and versatile approaches to rapid and efficient syntheses of pharmacologically relevant core structures. These include: combination of both solution- and solid-phase processes in the synthesis of pyrazolo[1,5-a]-[1,3,5]-triazin-4-ones and pyrazolo[1,5-a]-[1,3,5]-triazines; parallel, multi-generation synthesis of highly functionalized heterocyclic compounds in solution; a multi-step synthesis of 2,5-diketopiperazine on solid support taking advantage of a bicyclic ?-lactam scaffold, and a combined solid- and solution-phase synthesis of a new class of 2,4-diaminothiazoles.