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
Title |
Year |
Author |
Number |
METHOD OF PRODUCING LOSARTAN |
2006 |
- Vang Japing
- Li Jongang
- Li Julin
- Zheng Guodzhun
- Li Ji
|
RU2412940C2 |
NITROGEN-CONTAINING HETEROCYCLIC AROMATIC COMPOUND, METHOD FOR PRODUCTION THEREOF, PHARMACEUTICAL COMPOSITION BASED THEREON AND USE THEREOF |
2017 |
- Xu, Zusheng
- Lou, Yangtong
- Chen, Li
|
RU2729999C1 |
METHOD OF PREPARING 4A,5,9,10,11,12-HEXAHYDRO-6H- BENZOFURO (3A,3,2-ef/2/BENZAZEPINE DERIVATIVES AND INTERMEDIATE COMPOUNDS |
1995 |
- Laslo Chollner
- Jokhannes Frelikh
- Ul'Rikh Jordis
- Bernkhard Kjuenburg
|
RU2146258C1 |
PHARMACEUTICAL FORMULATIONS AND METHODS INCLUDING COMBINATIONS OF 2-ALKYLIDEN DERIVATIVES OF 9-NOR-VITAMIN D AND BISPHOSPHONATE |
2004 |
|
RU2326695C2 |
BENDAMUSTINE DERIVATIVES, RELATED COMPOUNDS AND THEIR MEDICAL APPLICATION FOR TREATING CANCER |
2013 |
- Shikkaneder Khelmut
- Shikkaneder Kristian
- Bushauer Armin
- Bernkhardt Gyunter
- Khuber Shtefan
- Limmert Mikhael
- Lubbe Matias
- Khofmajer Garald
|
RU2695383C2 |
SERINE/THREONINE KINASE INHIBITORS |
2013 |
- Blejk Dzhejms F.
- Chikarelli Mark Jozef
- Gerri Rustam Ferdinand
- Gaudino Dzhon
- Grina Dzhonas
- Moreno Devid A.
- Mor Peter Dzh.
- Ren Li
- Shvarts Dzhejkob
- Chen Khuejfen
- Robardzh Kirk
- Chzhou Ajkhe
|
RU2650501C2 |
METHOD OF STEREOSELECTIVE SYNTHESIS OF HETEROBICYCLIC ALCOHOL ENANTIOMER, INTERMEDIATE COMPOUNDS AND METHODS OF THEIR SYNTHESIS |
1997 |
- Bejzer Nikolas
- Krjuse Kris Gerrit
- Shenk Klara Marija
- Shadid Belal
|
RU2185379C2 |
DERIVATIVE OF PYRIMIDINE AND A FIVE-MEMBERED NITROGEN-CONTAINING HETEROCYCLE, METHOD FOR PRODUCTION AND MEDICAL APPLICATIONS THEREOF |
2019 |
- Zou Hao
- Li Zhengtao
- Wang Yuanhao
- Yu Jian
- Zhu Wei
|
RU2775229C1 |
INHIBITORS OF TH2-DIFFERENTIATION |
2000 |
- Arimura Akinori
- Kavada Kendzhi
|
RU2230551C2 |
DERIVATIVES OF 2-ALKYLIDEN-19-NOR-VITAMIN D FOR TREATMENT OF WEAKNESS, MUSCULAR INVOLVEMENT OR SARCOPENY |
2004 |
|
RU2326674C2 |