Ligand-free Suzuki coupling of arylboronic acids with methyl (E)-4-bromobut-2-enoate: synthesis of unconventional cores of HIV-1 protease inhibitors.
An effective ligand-free Suzuki coupling protocol to unite methyl (E)-4-bromobut-2-enoate with several arylboronic acids has been accomplished. Thus, a number of variously functionalized methyl 4-arylcrotonates have been achieved in high to excellent yields under mild conditions. This method enables the preparation of diverse aryl-substituted cores of HIV-1 protease inhibitors.
Dipartimento di Chimica Antonio Mario Tamburro, Università Degli Studi della Basilicata, Viale dell'Ateneo Lucano 10, 85100, Potenza, Italy.
Lucia
L
Chiummiento
Maria
M
Funicello
Paolo
P
Lupattelli
Francesco
F
Tramutola
D001897:Boronic Acids / Q000737:chemistry*; D002384:Catalysis; D020650:Combinatorial Chemistry Techniques; D003437:Crotonates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D015394:Molecular Structure; D010165:Palladium / Q000737:chemistry
D001897:Boronic Acids; D003437:Crotonates; D017320:HIV Protease Inhibitors; D010165:Palladium