METHOD OF PRODUCING CANDESARTAN Russian patent published in 2010 - IPC C07D403/10 C07D235/26 

Abstract RU 2407741 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing candesartan or a protected form of candesartan, candesartan salt or candesartan ester using a catalyst or several catalysts preferably containing one or more transition metals, and one or more of the following solvents: tetrahydrofuran (THF), THF/NMP (N-methylpyrrolidone), Et2O, DME (dimethoxy ethane), benzene, toluene, involving the following steps: (a) supply and reaction of a compound of formula (I), where R denotes hydrogen, unsubstituted or substituted alkyl or aryl radical, preferably methyl or (cyclohexyloxycarbonyloxy)ethyl, Y1 denotes a group capable of a coupling reaction into which Y2 comes in to form a C-C bond, with a compound of formula (II), having group Y2, where R1 is selected from a group comprising hydrogen, tert. Butyl and triphenylmethyl, preferably triphenylmethyl, to form candesartan, a protected form of candesartan or candesartan ester or candesartan cilexetil or some other candesartan ester, where (i) Y1 denotes B(OR4)2, where each of the radicals R4 independently denotes hydrogen, alkyl, aryl or alkylaryl, preferably hydrogen, and Y2 denotes a halogen, preferably bromine, or (and) Y denotes a halogen, preferably bromine,and Y2 denotes B(OR4)2, where each of radicals R4 independently denotes hydrogen, alkyl, aryl or alkylaryl, preferably hydrogen, and if necessary, (b) conversion to candesartan, candesartan cilexetil or salt.

.

EFFECT: novel method for producing candesartan with high output.

24 cl, 3 dwg, 1 tbl, 9 ex

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RU 2 407 741 C2

Authors

Vang Japing

Li Jongang

Di Julin

Zheng Guodzhun

Li Ji

Kekher Shtefan

Dates

2010-12-27Published

2005-12-15Filed