135050-95-2Relevant articles and documents
Preparation method of olmesartan medoxomil
-
Paragraph 0033; 0034; 0035; 0036; 0037; 0038, (2017/02/09)
The invention discloses a preparation method of olmesartan medoxomil. The preparation method comprises the following steps of using 4-bromobenzaldehyde as a starting raw material, performing Suzuki coupling reaction with 2-(2'-triphenylmethyl tetrazole-5-yl)borophenylic acid (III), and reducing by NaBH4 (sodium borohydride), so as to obtain an olmesartan medoxomil intermediate of N-triphenylmethyl-5-(4'-hydroxymethyl biphenyl-2-yl)tetrazole (IV); directly reacting the intermediate (IV) and 2-propyl-4-(1-hydroxy-1-methylethyl)imidazole-5-carboxylic acid ethyl ester, so as to obtain a compound VI; performing hydrolysis, esterification and deprotection, so as to obtain the olmesartan medoxomil. Compared with the prior art, the preparation method has the advantages that the obtaining of raw materials is easy, the amount of byproducts is fewer, the reaction line is shortened, the reaction condition is mild, the operation is simple, the total yield of product is improved, and the preparation method is suitable for industrialized production.
Model reactions targeted at the synthesis of carbon-14 labeled CI-996, a potent antagonist of angiotensin II receptor (1)
Ekhato,Huang
, p. 213 - 220 (2007/10/02)
A reaction sequence suitable for the preparation of an analog of 2-propyl-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl-4-[2-(tr ifluoroacetyl)-1H-pyrrol-1-yl]-1H-imidazole-5-carboxylic acid, with 14C at the methylene bridge was developed. The would-be labeled fragment (12) was derived from 4-iodobenzenemethanol (6) which itself was constructed from 1,4-dibromobenzene by the application of silicon chemistry. Pd(o) catalyzed coupling of TBDMS protected 6 and a tetrazole borate 10 gave the compound 12 which upon further transformation to the mesylate 13, N-alkylated an imidazole to furnish target compound.