73833-13-3

Upstream product

• 21606-04-2 methyl 2-carboxy-3-nitrobenzoate 
• 603-11-2 3-nitrophthalic acid 
• 13365-26-9 dimethyl 3-nitrophthalate 

Downstream Products

• 52682-10-7 3-nitro-phthalic acid methyl ester-⁽¹⁾-menthyl ester-⁽²⁾; 3-nitro-phthalic acid methyl ester-⁽¹⁾-l-menthyl ester 
• 7335-60-6 2-benzoyl-3-nitro-benzoic acid 
• 7335-77-5 6-nitro-o-benzoylbenzoic acid 
• 57113-90-3 methyl 2-(N-tert-butoxycarbonylamino)-3-nitrobenzoate 
• 136304-78-4 methyl 3-amino-2-[[(2'-cyanobiphenyl-4-yl)methyl]amino]benzoate 
• 136285-69-3 ethyl 3-amino-2-<<(2'-cyanobiphenyl-4-yl)methyl>amino>benzoate 
• 139481-37-1 methyl 3-amino-2-<<<2'-(methoxycarbonyl)biphenyl-4-yl>methyl>amino>benzoate 
• 139481-28-0 methyl 2-<<2'-cyanobiphenyl-4-yl)methyl>amino>-3-nitrobenzoate 
• 139481-33-7 methyl 1-<(2'-cyanobiphenyl-4-yl)methyl>-2,3-dihydro-2-oxo-1H-benzimidazole-7-carboxylate 
• 139481-34-8 methyl 2-chloro-1-<(2'-cyanobiphenyl-4-yl)methyl>-1H-benzimidazole-7-carboxylate 
• 136304-69-3 ethyl 1-<(2'-cyanobiphenyl-4-yl)methyl>-2-methyl-1H-benzimidazole-7-carboxylate 
• 139481-47-3 3-(2'-Cyano-biphenyl-4-ylmethyl)-2-methoxy-3H-benzoimidazole-4-carboxylic acid methyl ester 
• 139481-48-4 3-(2'-Cyano-biphenyl-4-ylmethyl)-2-methylamino-3H-benzoimidazole-4-carboxylic acid methyl ester 
• 139481-43-9 ethyl 1-<(2'-cyanobiphenyl-4-yl)methyl>-2-mercapto-1H-benzimidazole-7-carboxylate 

Relevant academic research and scientific papers

Synthesis Method for Candesartan Cilexetil Intermediate

A synthesis method for a candesartan cilexetil intermediate represented by formula (II) is provided. The method includes (1) dissolving a compound represented by formula (IV) to an aprotic solvent to obtain a first mixed solution, and dissolving a phase transfer catalyst and an azidation reagent to water to obtain a second mixed solution; (2) dropping the first mixed solution to the second mixed solution for azidation reaction, and after the reaction is ended, standing and layering same to obtain an organic phase containing a compound represented by formula (V); (3) dropping the obtained organic phase containing the compound represented by formula (V) to tertiary butyl alcohol for rearrangement reaction, and after the reaction is ended, concentrating same to obtain a solid or oily material, then adding a crystallizing solvent to the obtained solid or oily material for recrystallization, and separating same to obtain a crystal.

A 2 - ethoxy benzimidazole - 7 - carboxylic acid methyl ester

The invention discloses a synthesis method of 2-ethoxy benzimidazole-7-carboxylic acid methyl ester. The problem that an existing process is not high in content and is very low in yield is solved. According to the synthesis method, 3-nitryl phthalic acid is used as a raw material, rearrangement is performed in a water solution after methyl esterification, acylation and re-nitridation, then tin powder is adopted to perform reduction and loop closing so as to obtain the 2-ethoxy benzimidazole-7-carboxylic acid methyl ester. By the adoption of the synthesis method, produced impurities are very little, the content is high, and the yield is also high.

PROCESS FOR PREPARATION OF CANDESART AN CILEXETIL SUBSTANTIALLY FREE OF DES-CANDESARTAN CILEXETIL IMPURITY

The present invention provides a process for preparation of candeartan cilexetil substantially free of 2,3-dihydro-2-oxo-3-[[2'-(2H-tetrazol-5-yl)[l,l-biphenyl]-4- yl]methyl]-l-[[(cyclohexyloxy)carbonyl]oxy]ethylester-lH-benzimidazole-7- carboxylate (des-candesartan cilexetil) impurity.

PROCESS FOR PREPARING CANDESARTAN CILEXETIL

A process for preparing candesartan cilexetil.

METHOD FOR PRODUCTION OF CANDESARTAN

The invention relates to novel methods for the production of Candesartan, or a protected form of Candesartan, a Candesartan salt or ester, compounds of application in said method, methods for production thereof, use thereof in said method, a novel polymorph of Candesartan cilexetil, a method for production and use thereof for production of a medicament.

Nonpeptide Angiotensin II Receptor Antagonists. Synthesis and Biological Activity of Benzimidazolecarboxylic Acids

A series of 2-substituted-1--1H-benzimidazole-7-carboxylic acids was prepared from the key intermediate 3-amino-2-amino>benzoate (6a-c) in order to clarify the structure-activity relationships of various analogues of 2-butyl-1-methyl>-1H-benzimidazole-7-carboxylic acid (CV-11194), a potent and long acting angiotensin II (AII) receptor antagonist.The AII antagonistic activity of the benzimidazoles was investigated by in vitro assays, which included an AII receptor binding assay and AII-induced vasocontraction assay, as well as by in vivo assays such as an AII-induced pressor response in rats.Most of the benzimidazoles showed high affinity for the AII receptor (IC50 value, 10-6-1--7 M) and inhibited the AII-induced pressor response at 1 or 3 mg/kg po, and the effects were more potent than those of CV-11194 and DuP 753.The structure-activity relationship studies on the binding affinity and the inhibition of AII-induced pressor response suggested that straight chains of a certain length (e.g., ethoxy groups, ethyl groups) were the best as substituents at the 2-position and that their steric factors, lipohilicity, and electronic effects affected the potency of the AII antagonistic action.Both a carboxyl group at the 7-position and a tetrazole ring at the 2'-position were particularly important for potent and orally active AII antagonistic activity and a long-acting hypotensive effect.The representative compound, 2-ethoxy-1-methyl>-1H-benzimidazole-7-carboxylic acid (26b, CV-11974), inhibited the specific binding of AII to bovine adrenal cortical membrane with an IC50 value of 1.1*10-7 M.The AII-induced contraction of rabbit aortic strips was antagonized by CV-11974 (IC50 value, 3.0*1--10 M).Oral administration of CV-11974 to conscious normatensive rats at 1 mg/kg resulted in long-lasting inhibition of the AII-induced pressor response.CV-11974 at 0.1-1 mg/kg iv reduced blood pressure dose-dependently in spontaneously hypertensive rats.

Aspects of Tautomerism: Part X - Neighbouring Group Effects on the Structure and Reactivity Patterns of Acid Chlorides

The influence of neighbouring groups on the structure and reactivity patterns of over one hundred acid chlorides derived from γ- and δ-keto acids, 1,2- and 1,3-dicarboxylic acid half-esters and diacid chlorides have been examined.Contrary to reports in the literature, text books and monographs, evidence has been obtained for the non-existence of tautomerism between the isomeric pairs of either acid chlorides or half-ester acid chlorides.ce.