METHOD FOR PREPARING 1-(2-HALOGENOBIPHENYL-4-YL)-CYCLOPROPANECARBOXYLIC ACID DERIVATIVES Russian patent published in 2015 - IPC C07C51/09 C07C17/14 C07C253/14 C07C253/30 B01J23/44 C07C255/46 C07C255/35 C07C61/40 

Abstract RU 2540076 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for preparing a compound of formula

,

wherein R represents one or more groups optionally specified in halogen atoms, and n makes 1 or 2; or its pharmaceutically acceptable salts. The method involves the following stages: (1) reacting a compound of formula

,

wherein X' is specified in chlorine, bromine, iodine and triflate group (CF3SO3), with 1,2-dibromethane to form a compound of formula

,

(2) binding in the presence of a palladium catalyst representing mixture of Pd(OAc)2 and triphenylphosphine, a compound of formula (V) to a compound of formula ,

wherein R is such as specified above to form a compound of formula ;

(3) hydrolysing the compound of formula (VII) to form a compound of formula (IA). The invention also refers to a method for preparing a pharmaceutical composition involving the above stages (1)-(3) and the additional stage involving mixing to one or more pharmaceutically acceptable excipients.

EFFECT: method enables preparing the high-yield products.

9 cl, 5 ex

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RU 2 540 076 C2

Authors

Pivetti Fausto

Fornaretto Maria Gioia

Re Marco

Dates

2015-01-27Published

2010-07-22Filed