Patent ID: 6774229
Filing Date: 2004-08-10
Classification: A61P,C07D

Abstract:
Process for the preparation of heterocycles comprising reacting the following components:(i) a propargyl derivative of the general structural formula I â€ƒwherein Het is an optionally substituted hetero atom and A is a substituted or unsubstituted aromatic entity, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene, an olefin, an alkyne, a nitrile, or an acceptor group chosen from among carboxylic acid, ester, amide, imide or hydrazide; sulphonic acid, ester, amide, imide or hydrazide; phosphonic acid, ester, amide, imide or hydrazide; boronic acid, ester, amide, imide or hydrazide; cyano; heto; formyl; imine; trifluoromethyl; trialkylammonium; trialkylsilyl; &eegr;6-phenyl(Cr(CO)3; and &eegr;6-6-phenylFe+cyclopentadienyl complex; (ii) a compound of the general structural formula II Bâ€”Xâ€ƒâ€ƒII, â€ƒwherein B is an electron-deficient substituted or unsubstituted aromatic entity, an electron-deficient substituted or unsubstituted heteroaromatic entity with or without an acceptor group, an electron-deficient olefin and/or alkyne, and X is a leaving group; (iii) a nucleophile of the general structural formula III Yâ€”Cnâ€”Zâ€ƒâ€ƒIII, â€ƒwherein Y and/or Z, each independently of the other, is an amino group, thio group (mercapto group), seleno group, telluro group, hydroxy group (alcohol group); C is a substituted or unsubstituted C atom or atoms, where double or single bonds may be represent between said C atoms, and n=0-10 in a one-pot reaction by cyclocondensation to form one or more 5- to 10-membered heterocyclic, aromatic or non-aromatic ring systems.