Processes for producing epoxytriazole derivative and...

Details Processes for producing epoxytriazole derivative and... Processes for producing epoxytriazole derivative and...

C - Chemistry, Metallurgy

07

D

C07D 301/02 (2006.01) C07C 45/67 (2006.01) C07D 249/08 (2006.01) C07D 303/14 (2006.01) C07D 303/16 (2006.01) C07D 405/06 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2489611

An epoxytriazole derivative (V) useful as an intermediate for anti-fungal agents and an intermediate therefor having high quality can be produced economically and efficiently by the following industrial means. A compound of the following formula (I) is reacted with trimethyloxosulfonium salt and the like in the presence of a base to give compound (II), this compound is converted to compound (IV), and this compound is reacted with 1,2,4-triazole in the presence of a base. (see formula I) (see formula II) (see formula IV) (see formula V) wherein Ar is a phenyl group optionally substituted by 1 to 3 halogen atom(s) or trifluoromethyl group, R is a hydrogen atom or lower alkyl group, and X is a leaving group.

Dans cette invention, un compos~ repr~sent~ par la formule (I) est amen~ ~ r~agir avec un sel trim~thyloxosulfonium notamment, en pr~sence d'une base, pour produire un compos~ (II). Le compos~ (II) est converti en un compos~ (IV). Le compos~ (IV) est amen~ ~ r~agir avec du 1,2,4-triazole en pr~sence d'une base. Ainsi, un d~riv~ d'~poxytriazole de haute qualit~ (V) utile comme interm~diaire pour des agents antifongiques et un interm~diaire de haute qualit~ pour ce d~riv~ peuvent Útre produits efficacement ~ faible coÛt par un moyen industriel. Dans ces formules, Ar repr~sente ph~nyle ~ventuellement substitu~ par 1 ~ 3 atomes d'halog­ne ou par trifluorom~thyle ; R repr~sente hydrog­ne ou alkyle inf~rieur ; et X repr~sente un groupe partant.

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