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US 6,646,128 B2Granted
Process for preparing heterocyclo-alkylsulfonyl pyrazole derivatives
AssigneePfizer Inc.
InventorsDennis E. Bourassa, Michael J. Castaldi, David B. Ripin
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Abstract
The invention relates to processes for preparing compounds of formula 1: as well as intermediates useful in such processes, wherein R1-R4 are as defined herein. The compounds of formula 1 are useful in the treatment or alleviation of inflammation and other inflammation associated disorders.
Claims33
A process for preparing a compound of the formula 1
- which comprises combining
- (a) a compound of formula 2
- (b) a compound of formula 3
- (c) one or more acids;
- (d) one or more water-miscible organic solvents;
- and
- (e) water;
- wherein
- R1 is phenyl optionally substituted by 1-3 substituents independently selected from the group consisting of halo, hydroxy, cyano, mercapto, (C1-C6)alkyl, (C2-C6)alkenyl, (C1-C6)alkoxy, —OCF3, (C1-C6)alkyl-S—, (C1-C6)alkyl-S(═O)—, (C1-C6)alkyl-SO2—, amino, (C1-C6)alkylamino, di[(C1-C6)alkyl]amino, H2N—(C═O)—, (C1-C6)alkyl-NH—(C═O)— and formyl;
- R2 is hydrogen, halo or (C1-C6)alkyl;
- R3 is (C1-C6)alkyl optionally substituted with one to three halo atoms;
- and
- R4 is (C1-C6)alkyl.
10 more elements
Dependencies are inferred from the claim text.