- Method for synthesizing olmesartan medoxomil intermediate impurities
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The invention relates to the field of medicines and in particular relates to a method for synthesizing olmesartan medoxomil intermediate impurities. The olmesartan medoxomil intermediate impurities respectively refer to an impurity C, an impurity D and an impurity F. The respective synthetic reaction equations of the impurities are shown in the followings. The method specifically comprises the following steps: (1) taking an intermediate I as a raw material, and performing reactive deprotection with acetic acid so as to obtain the impurity C; (2) hydrolyzing an initial material B {4-[2-(trityl tetrazol-5-yl)phenyl] benzyl bromide} in a reaction system so as to obtain the impurity D; and (3) hydrolyzing an intermediate II into carboxylic acid in the reaction system, thereby obtaining the impurity F. According to the synthetic method for preparing the impurities, disclosed by the invention, a high-purity reference substance is conveniently obtained, and due to the optimized process, production of the impurities is specifically controlled, so that the quality of the raw drugs is improved. The reaction equation of the impurity C is as shown in the specification. The reaction equation of the impurity D is as shown in the specification. The reaction equation of the impurity F is as shown in the specification.
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Paragraph 0033; 0037; 0038; 0039; 0042; 0046; 0047; 0048
(2017/07/21)
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- A process for the preparation of olmesartan
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The invention discloses a preparation method of Olmesartan Medoxomil. The method is used for synthesizing an important intermediate 4-[2-(2-triphenylmethyl tetrazole-5-yl) phenyl] benzyl bromide (a compound III) so as to prepare the compound Olmesartan Medoxomil. The method is high in yield, easy to separate and purify, simple to operate and suitable for industrial production.
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- Preparation of 5 - (4 the [...] -bromo methyl-2-biphenyl) - 1-trityl tetrazazole method
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The invention discloses a method for preparing 5-(4'-bromomethyl-2-biphenyl)-1-triphenyl methyl tetrazole. According to the method, 2-cyano biphenyl is used for replacing 2-cyano 4'-methyl biphenyl in the conventional process and is used as a starting material, and a target product, the 5-(4'-bromomethyl-2-biphenyl)-1-triphenyl methyl tetrazole, is obtained by means of hydroxymethylation, cyclization, protection, and substitution reaction. The method has the advantages of low cost of the raw materials, convenience for recovery of solvent, less comprehensive pollution and the like and is suitable for industrialized production.
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Paragraph 0040; 0043
(2017/02/24)
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- Imidazole derivatives having a II antagonist activity
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Imidazole derivatives having A II antagonist activity, of Formula I, the processes for the preparation thereof, pharmaceutical compositions containing them and the use thereof as therapeutic agents. The described compounds having A II antagonist activity
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- New nonpeptide angiotensin II receptor antagonists. 2. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4- (biphenylylmethoxy)quinoline derivatives
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A novel series of nonpeptidic angiotensin II (AII) receptor antagonists is reported, derived from linkage of the biphenylcarboxylic acid or biphenylyltetrazole moiety found in previously described antagonists via a methyleneoxy chain to the 4-position of
- Bradbury,Allott,Dennis,Fisher,Major,Masek,Oldham,Pearce,Rankine,Revill,Roberts,Russell
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p. 4027 - 4038
(2007/10/02)
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