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

摘要

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 oran aromatic heterocyclic group; or A is a cyclic group R A1R A2C-CR A3R A4wherein R A2 and R A3, together with the carbon atoms to which they areat-tached form an optionally substituted saturated or unsaturated carbocyclicorheterocyclic group and R A1 and R A4 are as defined below or together forma bond; or A is a non-cyclic group R A1R A2C-CR A3R A4 wherein R A1 - R A4are 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; andR A1 - -R14, W, X and Y may be the same or different and each are selectedfromhydrogen, optionally substituted alkyl, optionally substituted alkenyl, option-allysubstituted alkynyl, optionally protected hydroxy, optionally substitutedamino, optionally substituted alkoxy, optionally substituted alkenoxy, option-allysubstituted alkynoxy, optionally substituted aryl, optionally substitutedheterocyclyl, carboxy, carboxy ester, carboxamido, acyl, acyloxy, mercapto,optionally substituted alkylthio, halogen, nitro, sulfate, phosphate andcyano,or W and X, together with the nitrogen and carbon atoms to which theyare attached, form a saturated or unsaturated nitrogen containing heterocyclicgroup which may be optionally substituted or optionally fused to a satu-ratedor unsaturated carbocyclic group, aryl group or heterocyclic group; orpharmaceutically acceptable derivatives and salts, racemates, isomers and/ortautomers thereof.