Patent ID: 6951943

Claim:
A process for the preparation of a compound of formula 1): wherein: Ar 1 is an optionally substituted aromatic or heteroaromatic group; L 2 is a linker group selected from —N(R 4 )—, —CON(R 4 )— and —S(O) 2 N(R 4 )—; R 4 is a hydrogen atom or an a optionally substituted straight or branched C 1-6 alkyl group; R 1 is a carboxylic acid (—CO 2 H) or an acyclic or cyclic carboxylic acid ester, an amide, tetrazole, phosphonic acid, phosphinic acid, sulphonic acid, sulphinic acid, boronic acid, or an acylsulphonamide group; R 2 is a hydrogen atom or a C 1-6 alkyl group; R x , R y and R z , which may be the same or different, are each -L 1 (Alk 1 ) n (R 3 ) v , or R z is -L 1 (Alk 1 ) n (R 3 ) v and R x and R y are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; L 1 is a covalent bond or —O—, —S—, or —Se— atom or an —C(O)—, —C(O)O—, —OC(O)—, —C(S)—, —S(O)—, —S(O) 2 —, —N(R 8 )—, —CON(R 8 )—, —OC(O)N(R 8 )—, —CSN(R 8 ), —N(R 8 )CO—, —N(R 8 )C(O)O—, —N(R 8 )CS—, —S(O) 2 N(R 8 )—, —N(R 8 )S(O) 2 —, —N(R 8 )O—, —ON(R 8 )—, —N(R 8 )N(R 8 )—, —N(R 8 )CON(R 8 )—, —N(R 8 )CSN(R 8 )—, or —N(R 8 )SO 2 N(R 8 )— group; R 8 is a hydrogen atom or optionally substituted straight or branched C 1-6 alkyl group; Alk 1 is an optionally substituted aliphatic chain or an optionally substituted heteroaliphatic chain containing one to four —O— or —S— atoms or —C(O)—, —C(O)O—, —OC(O)—, —C(S)—, —S(O)—, —S(O) 2 —, —N(R 8 )—, —CON(R 8 )—, —OC(O)N(R 8 )—, —CSN(R 8 ), —N(R 8 )CO—, —N(R 8 )C(O)O—, —N(R 8 )CS—, —S(O) 2 N(R 8 )—, —N(R 8 )S(O) 2 —, —N(R 8 )O—, —ON(R 8 )—, —N(R 8 )N(R 8 )—, —N(R 8 )CON(R 8 )—, —N(R 8 )CSN(R 8 )—, or —N(R 8 )SO 2 N(R 8 )— groups that interrupt or are at the terminus of the aliphatic chain; R 3 is a hydrogen or halogen atom or group selected from —OR 3a , —SR 3a , —CN and an optionally substituted cycloaliphatic, heterocycloahiphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group; R 3a is hydrogen atom or an optionally substituted straight or branched C 1-6 alkyl group or C 3-8 cycloalkyl group; n is zero or the integer 1; and v is the integer 1, 2 or 3; provided that when n is zero and L 1 is a covalent bond, v is the integer 1; and the salts, solvates, hydrates and N-oxides thereof; which comprises reacting a compound of formula (2): wherein: Q a is a group —N(R 4 )H; and the salts, solvates, hydrates and N-oxides thereof; with a compound Ar 1 W wherein W is a group selected from X 1 , —COX 2 and —SO 2 X 3; X 1 is a leaving atom or group; X 2 is a halogen atom or a —OH group; and X 3 is a halogen atom.