Patent ID: 8034958

Claim:
A method of preparation of compound of formula (I) wherein X is —CA 1 NR 5 R 6 or —CA 1 -R 8 ; A 1 is oxygen, sulfur or —NR 9 ; R 1 is hydrogen, alkyl, aryl or —CH 2 —R 1a wherein R 1a is aryl, halogen, hydroxy, amino, nitro or cyano; R 3 is hydrogen, halogen, thiol, nitro, nitrooxy, cyano, azido, carboxy, amido, sulfonic acid, sulfonamide, alkyl, alkenyl, alkynyl, ester, ether, aryl, tetrazolyl, thiazolyl, thienyl, furyl, pyrrolyl, pyridinyl, alkynyloxy, acyloxy, oxyester, oxyamido, alkylsulfonyloxy, alkylsulfinyloxy, arylsulfonyloxy, arylsulfinyloxy, aryloxy, aralkoxy, alkylthio, alkenylthio, alkynylthio, arylthio, formyl, acetyl, propionyl, isobutyryl, valeryl, lauroyl, heptanedioyl, cyclohexanecarbonyl, crotonoyl, furmaroyl, acyloyl, benzoyl, naphtoyl, 4-carboxybutanoyl, oxalyl, ethoxalyl, cysteinyl, oxamoyl, alkylsulfonyl, alkenylsulfonyl, alkynylsulfonyl, arylsulfonyl, alkylsulfinyl, alkenylsulfinyl, alkynylsulfinyl or arylsulfinyl; R 3a is hydrogen, halogen, alkyl, alkenyl, alkynyl or aryl; R 5 , R 6 and R 9 are the same or different and each is independently hydrogen, hydroxy, alkyl, aryl, alkoxy, alkenyloxy, alkynyloxy, acyloxy, oxyester, oxyamido, alkylsulfonyloxy, alkylsulfinyloxy, arylsulfonyloxy, arylsulfinyloxy, aryloxy or arylakoxy; and R 8 is hydrogen, hydroxy, thiol, halogen, alkyl, aryl, alkylthio, alkenylthio, alkynylthio; with the provisos that at least one of R 3 and R 3a is other than hydrogen; and that when the compound is a mixture of all possible isomers, X is —CONR 5 R 6 and R 1 is hydrogen, methyl, ethyl or propyl then R 3 and R 3a substitution is other than mono-, di-methyl or mono-ethyl; and that when R 1 and R 3a are both hydrogen and X is —CONR 5 R 6 then R 3 is different from carboxy, ester, amido, substituted oxo-pyrrolidine, alkynyloxy, acyloxy, oxyester, oxyamido, alkylsulfonyloxy, alkylsulfinyloxy, arylsulfonyloxy, arylsulfinyloxy, aryloxy, aralkoxy, methyl, naphtyl, phenyl optionally substituted by oxy derivatives or in the para position by an halogen atom; which comprises cyclisation of a compound of formula (AA-II) wherein R 1 , R 3 , R 3a and X are as defined above for compound of formula (I) and Q 1 together with the oxygen to which it is attached is a leaving group.