675882-71-0Relevant articles and documents
Synthesis method of telmisartan intermediate
-
Paragraph 0011; 0014-0019, (2021/05/01)
The invention discloses a synthesis method of a telmisartan intermediate, and belongs to the technical field of medicine synthesis. The preparation method comprises the following steps: by taking methyl 3-methyl-4-butyrylamino-5-nitrobenzoate as a starting material, carrying out reduction reaction in an alcohol solvent environment at the adding temperature of 40-70 DEG C and the reaction temperature of 40-70 DEG C under the joint participation of a nitro reducing agent and hydrazine hydrate, and filtering and spin-drying after the reaction is completed, so as to obtain 3-methyl-4-butyrylamino-5-aminobenzoic acid methyl ester. When the method is used for reducing nitro, the selectivity of reducing groups is high, raw materials are easy to obtain, pollution is small, and the requirement for equipment is low; and the method is low in cost, green, safe, simple and convenient to operate and easy to realize industrial production.
Novel preparation method of antihypertensive drug telmisartan intermediate
-
Paragraph 0085-0088, (2021/06/26)
The invention relates to an electric reduction preparation method of aminobenzoic acid represented by formula I and ester thereof. The preparation reaction of the method is shown in the description; and in the reaction formula, R is selected from hydrogen, a methyl group, an ethyl group, a benzyl group, a C3 or C4 straight-chain alkyl or branched-chain alkyl group, -NO2 is selected from 4-NO2 or 5-NO2, and Y is selected from H or 4-NHCOC3H7-n. The electroreduction preparation method of aminobenzoic acid and ester I thereof is characterized in that in a separated electrolytic cell, an acidic solution of nthe itrobenzoic acid and ester III thereof is taken as a catholyte; the voltage of a cathode working electrode relative to a reference electrode is 1.00-2.50 V; and an anolyte is an acidicsolution, the current density is 25.0-250.0 mA/cm, and the electrolysis temperature is 15-90 DEG C.
N-Phenyl indole derivatives as AT1 antagonists with anti-hypertension activities: Design, synthesis and biological evaluation
Zhu, Weibo,Bao, Xiaolu,Ren, He,Da, Yajing,Wu, Dan,Li, Fuming,Yan, Yijia,Wang, Li,Chen, Zhilong
, p. 161 - 178 (2016/04/05)
The design, synthesis, in vitro and in vivo evaluation of 6-substituted benzimidazole with 1, 4-disubsituted or 1, 5-disubsituted indole derivatives as novel angiotensin II receptor antagonists are outlined. Radioligand binding assays showed that several 6-substituted benzimidazole derivatives displayed high affinities binding to the angiotensin II type 1 receptor at the same order of magnitude to telmisartan. The biological evaluation on spontaneously hypertensive rats showed that 2-[4-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazole-1-yl]methyl]-1H-indol-1-yl]benzoic acid, 1c, could cause significant decrease on MBP in a dose dependent manner. Its maximal response lowered 53 mmHg of MBP at 5 mg/kg and 64 mmHg of MBP at 10 mg/kg after oral administration, and the significant antihypertensive effect lasted beyond 24 h, which was better than both losartan and telmisartan. A study designed to determine acute toxicity showed that 1c had low acute toxicity with no significant changes in the weight and no obvious untoward reactions. The encouraging results make 1c an effective and durable anti-hypertension drug candidate and deserve further investigation for therapeutic application.