Patent ID: 7932416

Claim:
A process for preparing an ortho-substituted pentafluorosulfanylbenzene of Formula (I): comprising reacting a pentafluorosulfanylbenzene with an electrophile under electrophilic aromatic substitution conditions selected from halogenation chlorosulfonation, sulfonation and nitration to effect substitution on the position ortho to said pentafluorosulfanyl on the benzene ring wherein: R1 is: Cl, Br, I, —SO 2 R6, or NO 2 ; R2 and R4 are, each independently, hydrogen, F, Cl, Br, I, —CN, NR9R10, —OR11, —SR12, —COR13, —(SO r ) s —(CH 2 ) t —(CF 2 ) u —CF 3 , alkyl having 1 to 6 carbon atoms, or cycloalkyl having 3 to 8 carbon atoms, wherein 1 to 4 hydrogen atoms in said alkyl or cycloalkyl may be replaced by fluorine atoms, where q and r are, each independently, 1 to 2, s is 0 to 1, t is 0 to 4, u is 0 to 1; where at least one of the residues R2 and R4 is not hydrogen, Cl, CN, —COR13 or —(SO r ) s —(CH 2 ) t —(CF 2 ) u —CF 3 ; and where R9 and R10: (a) are each independently, —(CH 2 ) v —(CF 2 ) w —CF 3 , alkyl having 1 to 4 carbon atoms, alkylcarbonyl having 1 to 4 carbon atoms, or alkylsulfonyl having 1 to 4 carbon atoms, where v is 0 to 4 and w is 0 to 1; or (b) together with the nitrogen atom bearing them, form a heterocycle of Formula (III): where X and Y are, each independently, CO or SO 2 ; and where R11 and R12 are, each independently, —(CH 2 ) v —(CF 2 ) w —CF 3 , hydrogen, alkyl having 1 to 4 carbon atoms, alkylcarbonyl having 1 to 4 carbon atoms, or alkylsulfonyl having 1 to 4 carbon atoms where v is 0 to 4 and w is 0 to 1; and R13 is OH, alkyl having 1 to 6 carbon atoms or alkoxy having 1 to 6 carbon atoms; R3 is hydrogen, F, Cl, Br, I, —CN,—NO 2 , —COR14, —SO 2 CH 3 , alkyl having 1 to 6 carbon atoms, or —O x —(CH 2 ) y —CF 3 , where x is 0 to 1 and y is 0 to 3; and where R14 is OH, alkyl having 1 to 6 carbon atoms, alkoxy having 1 to 6 carbon atoms or —O aa —(CH 2 ) bb —CF 3 , where aa is 0 to 1 and bb is 0 to 3; R5 is: (a) hydrogen, F, Cl, Br, I, —CN, —SO 2 CH 3 , —O—(CH 2 ) ee —(CF 2 ) ff —CF 3 , —(SO gg ) hh —(CH 2 ) jj —(CF 2 ) kk —CF 3 , alkyl having 1 to 6 carbon atoms or cycloalkyl having 3 to 8 carbon atoms, where 1 to 4 hydrogen atoms in said alkyl or cycloalkyl may be replaced by fluorine atoms, where ee and ff are, each independently, 0 to 1, gg is 0 to 2, hh is 0 to 1, jj is 0 to 4, kk is 0 to 1; and optionally converting the compound of Formula (I) into a pharmaceutically acceptable salt.