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US 7,745,634 B2Granted
Process for preparing triazolones
AssigneeRoche Palo Alto LLC
InventorsHumberto Bartolome Arzeno, Gary M. Lee, Michael Martin, Keshab Sarma, Jiang Zhu
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Abstract
The present process provides a improved method for the preparation of alkylsulfanyl substituted triazoles 2 which are useful intermediates in a new process for the preparation of triazolones 20.
Claims8
A process for preparing a compound of formula 2 wherein Ar is phenyl substituted with 2 or 3 groups independently selected from halogen, cyano and C1-6 haloalkyl, Rf is hydrogen, and R1 and R3 are C1-10 alkyl,
- which process comprises the steps of:
- (a) contacting 4 with a strong base in an inert solvent to form the conjugate base of 4 and contacting said conjugate base with 6 to afford 8;
- (b) exposing 8 to conditions which result in hydrolysis of the ester and decarboxylation of the resulting carboxylic acid to afford 2.
Dependencies are inferred from the claim text.