ChemInform Abstract: Synthesis and Biological Evaluation of Ketorolac Analogues.

2
2002 pyrrole derivatives pyrrole derivatives R 0120 20 - 083 Synthesis and Biological Evaluation of Ketorolac Analogues. The synthesis of title compounds Ro114-1907 (VII), Ro113-8905 (XV), and Ro101-8244 (XXIII) involves hydroxyethyl-assisted regioselective benzoylation and Cu-mediated ring closure as key steps. The furan (XV) and the thiophene (XXIII) exhibit significant biological activity but are less potent than ketorolac (XXIV). — (LOPEZ, FRANCISCO J.; JETT, MARY-FRANCES; MU- CHOWSKI, JOSEPH M.; NITZAN, DOV; O’YANG, COUNDE; Heterocycles 56 (2002) 1, 91-95; Roche Biosci., Palo Alto, CA 94304, USA; EN) 1

Transcript of ChemInform Abstract: Synthesis and Biological Evaluation of Ketorolac Analogues.

Page 1: ChemInform Abstract: Synthesis and Biological Evaluation of Ketorolac Analogues.

2002 pyrrole derivatives

pyrrole derivativesR 0120

20 - 083Synthesis and Biological Evaluation of Ketorolac Analogues. —The synthesis of title compounds Ro114-1907 (VII), Ro113-8905 (XV), andRo101-8244 (XXIII) involves hydroxyethyl-assisted regioselective benzoylationand Cu-mediated ring closure as key steps. The furan (XV) and the thiophene(XXIII) exhibit significant biological activity but are less potent than ketorolac(XXIV). — (LOPEZ, FRANCISCO J.; JETT, MARY-FRANCES; MU-CHOWSKI, JOSEPH M.; NITZAN, DOV; O’YANG, COUNDE; Heterocycles56 (2002) 1, 91-95; Roche Biosci., Palo Alto, CA 94304, USA; EN)

1

Page 2: ChemInform Abstract: Synthesis and Biological Evaluation of Ketorolac Analogues.

2002 pyrrole derivatives

2