Patent ID: 7355040
Filing Date: 2008-04-08
Classification: A61P,C07D,Y02P

Abstract:
1. A process for the preparation of a compound of formula (II): comprising cyclizing a compound of formula (II): wherein in formulae (II) and (III), R 1 is hydrogen, methoxy or formamido; R wherein p is 0, 1, or 2; m is 0, 1 or 2; A 1 is (C 1-6 ) alkyl, substituted (C 1-6 ) alkyl, (C 3-6 ) cycloalkyl, cyclohexenyl, cyclohexadienyl, an aromatic group, a (C 1-6 ) alkylthio group, (C 1-6 ) alkyloxy; X 1 is a hydrogen or halogen atom, azido, tetrazolyl, hydroxy, acyloxy, amino, uerido, acylamino, heterocyclylamino, guanidino or acylureido group; A 2 is an aromatic group, a phenyl, 2,6-dimethoxyphenyl, 2-alkoxy-1-naphthyl, 3-arylisoxazolyl, or a 3-aryl-5-methylisoxazolyl group, a substituted alkyl group; a substituted dithietane; X 2 is a —CH 2 OCH 2 —, —CH 2 SCH 2 — or alkylene group; X 3 is an oxygen or sulphur atom; A 3 is an aryl or heteroaryl group, phenyl, substituted phenyl, furyl, aminothiazolyl or aminothiadiazolyl in which the amino group is optionally protected; and A 4 is hydrogen, (C 1-6 )alkyl, (C 3-8 ) cycloalkyl, (C 3-8 ) cycloalkyl(C 1-6 )alkyl, (C 1-6 ) alkoxycarbonyl(C 1-6 ) alkyl, (C 2-6 ) alkenyl, carboxy(C 1-6 )alkyl, (C 2-6 ) alkynyl, aryl or (C 1-6 )alkyl substituted by up to three aryl groups; CO wherein R a is hydrogen, (C 1-6 ) alkyl, (C 3-7 ) cycloalkyl, methyl, or phenyl, R b is (C 1-6 )alkyl, (C 1-6 )alkyl, (C 1-6 )alkoxy, phenyl, benzyl, (C 3-7 ) cycloalkyl, (C 3-7 ) cycloalkyloxy, (C 1-6 )alkyl (C 3-7 )cycloalkyl, 1-amino (C 1-6 )alkyl, or 1-((C 1-6 )alkyl) amino (C 1-6 ) alkyl; or R a and R b together form a 1,2-phenylene group optionally substituted by one or two methoxy groups; R c represents (C 1-6 )alkylene optionally substituted with a methyl or ethyl group and R d and R e independently represent (C 1-6 )alkyl; R f represents (C 1-6 )alkyl, R g represents hydrogen or phenyl optionally substituted by up to three groups selected from halogen, (C 1-6 )alkyl, or (C 1-6 )alkoxy; Q is oxygen or NH; R h is hydrogen or (C 1-6 )alkyl; R i is hydrogen, (C 1-6 )alkyl optionally substituted by halogen, (C 2-6 )alkenyl, (C 1-6 )alkoxycarbonyl, aryl or heteroaryl; or R h and R i together form (C 1-6 )alkylene; R j represents hydrogen, (C 1-6 )alkyl or (C 1-6 )alkoxycarbonyl; and R k represents (C 1-8 )alkyl, (C 1-8 )alkoxy, (C 1-6 )alkoxy, (C 1-6 )alkoxy(C 1-6 )alkoxy or aryl, a group of the formula wherein R 5 is hydrogen, C 1-6 alkyl or phenyl; acetoxymethyl, pivaloyloxymethyl, α-acetoxyethyl, α-pivaloyloxyethyl, 1-(cyclohexylcarbonyloxy)prop-1-yl, and (1-aminoethyl)carbonyloxymethyl; ethoxycarbonyloxymethyl, α-ethoxycarbonyloxyethyl, propoxycarbonyloxyethyl; dialkylaminoalkyl, dimethylaminomethyl, dimethylaminoethyl, diethylaminomethyl or diethylaminoethyl; 2-(isobutoxycarbonyl)pent-2-enyl and 2-(ethoxycarbonyl)but-2-enyl; R X is S, SO, SO m is 1 or 2; and the dotted line indicates a double bond C2 and C3 or between C3 and C4 of formula II and Formula III, and where in formula (III) the substituent(s) R