Compounds

A process for preparing a compound of the formula:

• ##STR16## wherein p is 2;
• Ar is an optionally substituted phenyl;
• R.sub.4 is phenyl, naphth-1-yl or naphth-2-yl, or a heteroaryl, which is optionally substituted by one or two substituents, each of which is independently selected, and which, for a 4-phenyl, 4-naphth-1-yl, 5-naphth-2-yl or 6-naphth-2-yl substituent, is halogen, cyano, nitro, C(Z)NR.sub.7 R.sub.17,C(Z)OR.sub.16, (CR.sub.10 R.sub.20).sub.v COR.sub.12, SR.sub.5,SOR.sub.5, OR.sub.12, halo-substituted C.sub.1-4 alkyl, C.sub.1-4 alkyl, ZC(Z)R.sub.12,NR.sub.10 (Z)R.sub.16, or (CR.sub.10 R.sub.20).sub.v NR.sub.10 R.sub.20 and which, for other positions of substitution, is halogen, cyano, C(Z)NR.sub.13 R.sub.14, C(Z)OR.sub.3, (CR.sub.10 R.sub.20).sub.m "COR.sub.3, S(O).sub.m R.sub.3, OR.sub.3, halo-substituted C.sub.1-4 alkyl, C.sub.1-4 alkyl, CR.sub.10 R.sub.20).sub.m "NR.sub.10 C(Z)R.sub.3,NR.sub.10 S(O).sub.m 'R.sub.8, NR.sub.10 S(O).sub.m "NR.sub.7 R.sub.17, ZC(Z)R.sub.3 or (CR.sub.10 R.sub.20).sub.m "NR.sub.13 R.sub.14 ;
• n is an integer having a value of 1 to 10;
• v is 0, or an integer having a value of 1 or 2;
• m is 0, or the integer 1 or 2;
• m' is an integer having a value of 1 or 2;
• m" is 0, or an integer having a value of 1 to 5;
• Z is oxygen or sulfur:
• R.sub.3 is heterocyclyl, heterocyclylC.sub.1-10 alkyl or R.sub.8 ;
• R.sub.5 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or NR.sub.7 R.sub.17, excluding the moieties SR.sub.5 being SNR.sub.7 R.sub.17 and SOR.sub.5 being SOH:
• R.sub.7 and R.sub.17 is each independently selected from hydrogen or C.sub.1-4 alkyl or R.sub.7 and R.sub.17 together with the nitrogen to which they are attached form a heterocyclic ring of 5 to 7 members which ring optionally contains an additional heteroatom selected from oxygen, sulfur or NR.sub.15 ;
• R.sub.8 is C.sub.1-10 alkyl, halo-substituted C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.5-7 cycloalkenyl, aryl arylC.sub.1-10 alkyl, heteroaryl, heteroaryl, C.sub.1-10 alkyl, (CR.sub.10 R.sub.20).sub.n R.sub.20 (CR.sub.10 OR.sub.20).sub.11 (CR.sub.10 R.sub.20).sub.n S(O).sub.m R.sub.18, (CR.sub.10 R.sub.20).sub.n NHS(O).sub.2 R.sub.18, (CR.sub.10 R.sub.20).sub.n NR.sub.13 R.sub.14 ;
• wherein the aryl, arylalkyl, heteroaryl, heteroaryl alkyl may be optionally substituted:
• R.sub.9 is hydrogen, C(Z)R.sub.11 or optionally substituted C.sub.1-10 alkyl, S(O).sub.2 R.sub.18, optionally substituted aryl or optionally substituted aryl-C.sub.1-4 alkyl;
• R.sub.10 and R.sub.20 is each independently selected from hydrogen or C.sub.1-4 alkyl:
• R.sub.11 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, heterocyclyl, heterocyclyl C.sub.1-10 alkyl, aryl, arylC.sub.1-10 alkyl, heteroaryl or heteroaryl C.sub.1-10 alkyl;
• R.sub.12 is hydrogen or R.sub.16 ;
• R.sub.13 and R.sub.14 is each independently selected from hydrogen or optionally substituted C.sub.1-4 alkyl, optionally substituted aryl or optionally substituted aryl-C.sub.1-4 alkyl, or together with the nitrogen to which they are attached form a heterocyclic ring of 5 to 7 members which ring optionally contains an additional heteroatom selected from oxygen, sulfur or NR.sub.9 ;
• R.sub.15 is R.sub.10 or C(Z)-C.sub.1-4 alkyl:
• R.sub.16 is C.sub.1-4 alkyl, halo-substituted-C.sub.1-4 alkyl, or C.sub.3-7 cycloalkyl:
• R.sub.18 is C.sub.1-10 alky, C.sub.3-7 cycloalkyl, heterocyclyl, aryl, arylalkyl, heterocyclyl, heterocyclyl-C.sub.1-10 alkyl, heteroaryl or heteroarylalkyl;
• which process comprises reacting a compound of the formula ##STR17## wherein R.sub.4 is as defined above;
• with ArSO.sub.2 H, wherein Ar is as defined above in Formula (IV), and an acid catalyst, to yield a compound of Formula (IV).