METHOD OF SYNTHESISING SULFONYLHALOGENIDES AND SULFONAMIDES FROM SALTS OF SULFONIC ACIDS Russian patent published in 2012 - IPC C07C303/22 C07C303/38 C07C311/13 C07C309/81 C07D209/22 A61K31/405 

Abstract RU 2466983 C2

FIELD: chemistry.

SUBSTANCE: invention relates to obtaining cPLA2 inhibitors of formula (A1): , where Ar, R, z, R10, n1, n3, X2, R12, R13 and R14 have values, given in invention formula, or pharmaceutically acceptable salts of said compound, which includes reaction of corresponding compound of formula II: [Ar-(R)2-SO2-1]qM, where M and q have values, given in formula of invention, with reagent, carrying substituting halogen atom, in presence of catalytic amount of water and cocatalyst with formation of corresponding compound of formula III: Ar-(R)z-SO2-X, where X represents halogen; and reaction of formula III compound with corresponding compound of formula (B1): , where R12 represents phenyl, substituted with group -(CH2)n4-COOH, where carboxyl group is protected by protective group, with obtaining of sulfonamide; and if necessary, conversion of obtained compound into form of its pharmaceutically acceptable salt. In addition, claimed invention relates to novel intermediate compounds for obtaining cPLA2 inhibitors and to methods of obtaining intermediate compounds for obtaining cPLA2 inhibitors.

EFFECT: method improvement.

26 cl, 2 ex, 1 dwg

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RU 2 466 983 C2

Authors

Michalak Ronal Stehnli

Khelom Dzhen Luiza

Zel'Dis Dzhozef

Dates

2012-11-20Published

2006-07-20Filed