METHOD OF PRODUCING 1-(2-HALOGEN BIPHENYL-4-YL)-CYCLOPROPANE CARBOXYLIC ACID DERIVATIVES Russian patent published in 2013 - IPC C07C51/09 C07C17/14 C07C17/26 C07C253/14 C07C255/35 C07C57/62 C07C25/18 A61K31/192 C07C51/08 

Abstract RU 2502721 C2

FIELD: chemistry.

SUBSTANCE: invention relates to an improved method of producing a compound of formula , comprising the steps: 1) reacting a compound of formula , where X is a fluorine atom, and X1 is selected from a group consisting of chlorine, bromine and iodine atoms and a triflate group (CF3SO3), with a compound of formula , where R denotes two chlorine atoms, in the presence of a palladium catalyst to form a compound of formula ; 2) radical bromination of the compound of formula (IV) with N-bromosuccinimide in the presence of a catalytic amount of benzoyl peroxide to form a compound of formula ; 3) converting the compound of formula (V) to the corresponding nitrile derivative of formula ; 4) reacting the compound of formula (VI) with 1,2-dibromoethane to form a compound of formula ; and 5) hydrolysis of the compound of formula (VII) to obtain a compound of formula (Ia).

EFFECT: invention provides higher output of the compound with higher chemical purity without a chromatographic purification step.

8 cl, 5 ex

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RU 2 502 721 C2

Authors

Folle Benua

Bott Juber

Delakrua Toma

Pivetti Fausto

Dates

2013-12-27Published

2009-05-08Filed