Intermediates for pyrazolyl acetic acid derivatives
AssigneeSandoz Ltd.
InventorsErwin Waldvogel, Eugen Eichenberger
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AssigneeSandoz Ltd.
InventorsErwin Waldvogel, Eugen Eichenberger
Estimating the term…
The invention discloses a novel process for the preparation of a compound of formula II ##STR1## wherein R.sub.1 is C.sub.1-5 alkyl, R.sub.2 is hydrogen or C.sub.1-5 alkyl, and R.sub.3 is optionally substituted phenyl, comprising the reaction of a 4-hydroxypyrazole of formula III ##STR2## wherein R.sub.1 and R.sub.2 are as defined for formula II, with a benzylhalide of formula IV Hal--CH.sub.2 --R.sub.3 (IV) wherein Hal is halogen, preferably bromine or chlorine, and R.sub.3 is as defined for formula II, in the presence of a base. The invention further comprises a novel process for the preparation of the 4-hydroxypyrazole of formula III. The compounds of formulae II and III are intermediates for highly effective systemic fungicides of the class of pyrazolyl acetic acid derivatives.
Process for the preparation of a 4-hydroxypyrazole of formula III ##STR20## wherein R.sub.1 is C.sub.1-5 alkyl and R.sub.2 is hydrogen or C.sub.1-5 alkyl, comprising an intramolecular cyclization reaction of a compound of formula V ##STR21## wherein R.sub.1 and R.sub.2 are as defined for formula III, and A is a leaving group, at a temperature between +50.degree. C. and +200.degree. C.
Dependencies are inferred from the claim text.