New synthetic approaches to CNS drugs. A straightforward, efficient synthesis of tetrahydroindol-4-ones and tetrahydroquinolin-5-ones via palladium-catalyzed …

B Pita, CF Masaguer, E Raviña

Index: Pita, Beatriz; Masaguer, Christian F.; Ravina, Enrique Tetrahedron Letters, 2002 , vol. 43, # 44 p. 7929 - 7932

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Citation Number: 13

Abstract

Haloperidol (Haldol®, Jannsen 1959) is the prototype of a group of butyrophenone derivatives with a potent and antipsychotic activity. For some time, we have been interested in the utilization of cyclohexanedione I as a versatile synthon in the preparation of condensed heterocyclic systems as intermediates in the synthesis of butyrophenone-type CNS agents. In previous papers 1., , , 2. and 3. we have reported the preparation (and in most of them, the antipsychotic ...