| abstract |
IT HAS BEEN FOUND THAT INDOLAS 2-INSUSTITUIDAS OF THE STRUCTURAL FORMULA (IV) CAN BE SYNTHETIZED IN A GREAT QUANTITY THROUGH THE CLOSURE OF THE COUPLING / CATALYZED RING OF A 2-HALO OR 2-TRIFLUOROXYLED SILHONE-SILKED I-2 OF ACILO (II), FOLLOWING THE DESPROTECTION OF SILILO PROTECTIVE GROUPS. THE PROCESS OF THE INVENTION IS PARTICULARLY USEFUL FOR FORMING INDOLES CONTAINING LABEL SUBSTITUTES IN AN ACID ENVIRONMENT SUCH AS TRIAZOLA, ACETYL, QUETAL, CYANO, AND CARBAMATO, OR INDOLAS THAT HAVE A GOOD DEPARTURE GROUP IN THE POSITION OF BENCI. THE ADVANTAGES OF THE PROCESS ARE THAT IT DOES NOT REQUIRE THE USE OF PHOSPHINE OF TRIPHENYLL OR CHLORIDE OF TETRABUTILO OR CHLORIDE OF LITHIUM CHLORIDE. WHEN APPLIED TO SUBSTITUTED INDOLES, THE PROCESS ALSO ELIMINATES THE TRIAZOLILY POLYMERIZATION TREND IN THE SYNTHESIS OF LA INDOLA DE FISCHER. IN ADDITION, THE INVENTION IS DIRECTED TO NEW INTERMEDIARIES OF STRUCTURAL FORMULAS (V) AND (VI). |