PREPARATION OF FUSED POLYCYCLIC ALKALOIDS BY RING CLOSURE OFAZOMETHINE YLIDES, NOVEL COMPOUNDS THEREOF AND THEIR USE AS CHEMOTHERAPEUTIC AGENTS

• Main Authors: FLYNN, BERNARD LUKE, BANWELL, MARTIN GERHARDT
• Format: Patent
• Language: English; French
• Published: 22.12.2009
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

A method for the preparation of a compound of general Formula (I) comprising the step of cyclizing an azomethine ylide of general Formula (II) wherein A is a cyclic group being an optionally substituted aryl group or an aromatic heterocyclic group; or A is a cyclic group R A1R A2C-CR A3R A4 wherein R A2 and R A3, together with the carbon atoms to which they are at-tached form an optionally substituted saturated or unsaturated carbocycli c or heterocyclic group and R A1 and R A4 are as defined below or together form a bond; or A is a non-cyclic group R A1R A2C-CR A3R A4 wherein R A1 - R A4 are as defined below and R A2 and R A3 may optionally together form a bond; Z is a carbon or a heteroatom; n is selected from 0, 1, 2 or 3; and R A1 - -R14, W, X and Y may be the same or different and each are selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, opti on- ally substituted alkynyl, optionally protected hydroxy, optionally substituted amino, optionally substituted alkoxy, optionally substituted alkenoxy, optio n- ally substituted alkynoxy, optionally substituted aryl, optionally substituted heterocyclyl, carboxy, carboxy ester, carboxamido, acyl, acyloxy, mercapto, optionally substituted alkylthio, halogen, nitro, sulfate, phosphate and cyano, or W and X,together with the nitrogen and carbon atoms to which they are attached, form a saturated or unsaturated nitrogen containing heterocycl ic group which may be optionally substituted or optionally fused to a satu-rate d or unsaturated carbocyclic group, aryl group or heterocyclic group; or pharmaceutically acceptable derivatives and salts, racemates, isomers and/or tautomers thereof.