124750-67-0

Upstream product

• 57598-33-1 2-(2-methoxyphenyl)-4,4-dimethyl-2-oxazoline 
• 106-38-7 para-bromotoluene 
• 7148-03-0 o-tolylbenzoic acid 
• 79047-41-9 2-n-butyl-4-chloro-5-hydroxymethylimidazole 
• 114772-34-8 methyl 4'-methylbiphenyl-2-carboxylate 
• 84392-32-5 4,4-dimethyl-2-(4'-methyl-biphenyl-2-yl)-4,5-dihydrooxazole 
• 696-61-7 4-tolylmagnesium chloride 
• 873-32-5 2-Chlorobenzonitrile 
• 57246-71-6 methyl pentanimidate 
• 193140-43-1 (pentanimidoylamino)acetic acid 
• 110-59-8 pentanonitrile 
• 114772-53-1 2-Cyano-4'-methylbiphenyl 
• 83857-96-9 2-n-butyl-4-chloro-1H-imidazol-5-carboxaldehyde 
• 114772-54-2 4'-(bromomethyl)-1,1'-biphenyl-2-carbonitrile 

Downstream Products

• 114772-55-3 2-n-Butyl-4-chloro-1-[(2'-cyanobiphenyl-4-yl)-methyl]-5-(hydroxymethyl)imidazole 
• 124750-68-1 2-n-Butyl-4-chloro-5-cyano-1-[(2'-cyanobiphenyl-4-yl)methyl]imidazole 
• 124750-99-8 cozaar 
• 114798-26-4 2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]imidazole 
• 114798-26-4 lorsartan 
• 124750-99-8 losartan potassium 
• 114798-36-6 2-n-Butyl-4-chloro-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxaldehyde 
• 114798-36-6 EXP 3179 

Relevant academic research and scientific papers

Preparation method of losartan

The invention provides a preparation method of losartan. The losartan is prepared by reacting a cyano-containing intermediate as shown in a formula (I), which is described in the specification, with an azide reagent in toluene in the presence of a catalyst. After the reaction is finished, azide ions are removed through the following procedures: adding water to divide a reaction system into three layers, separating out a middle layer, adding n-butyl alcohol into the middle layer for dilution, and adding triphenylphosphine into the obtained diluted solution to remove the residual azide ions in the diluted solution. According to the preparation method, sodium nitrite is not needed, so formation of the genotoxic impurity nitrosamine is fundamentally eradicated; the obtained target losartan isgood in purity and high in yield; and the method is simple and convenient in preparation process, mild and easily controllable in operation conditions, good in safety, and suitable for large-scale industrial production.

Synthesis and evaluation of novel angiotensin II receptor 1 antagonists as anti-hypertension drugs

Three new angiotensin II receptor 1 antagonists, 1, 2 and 3 were designed, synthesized and evaluated. The AT1 receptor-binding assays in vitro showed that all the synthesized compounds had nanomolar affinity for the AT1 receptor. Fro

COMPOUNDS AS MODULATOR OF JAK-STAT PATHWAY, METHODS AND APPLICATIONS THEREOF

The present disclosure relates to compound of structural Formula I and a method for preparing said compounds. The disclosure further relates to a method of employing the Formula I compounds for modulation of Janus kinase-Signal Transducer and Activator of Transcription (JAK-STAT) pathway in cancer cells, and the corresponding use of compound of Formula I as anti-cancer agents.

An efficient and green synthetic route to losartan

A practical, efficient and green process for the preparation of losartan, an antihypertensive drug, has been developed with an overall yield of 58.6%. The key step is the synthesis of the two key intermediates 2-butyl-4-chloro-3H-imidazole-5-carbaldehyde (BCFI) and 2-cyano-4'-methyl biphenyl (OTBN). BCFI was synthesised from valeronitrile and acetyl chloride by three steps with an overall yield of 69%; OTBN was obtained in 86% yield by the coupling of o-chlorobenzonitrile with p-methylphenylmagnesium chloride in tetrahydrofuran in the presence of manganese chloride and chlorotrimethylsilane. The above route was successfully operated in at a pilot-plant operation.

An efficient, commercially viable, and safe process for preparation of losartan potassium, an angiotensin II receptor antagonist

An efficient, commercially viable and safe process for the preparation of losartan potassium, an antihypertensive drug substance, with an overall yield of 55.5% and ～99.9% purity (including five chemical reactions and two recrystallizations) and meeting all other regulatory requirements is described. Formation and control of all the possible impurities are also described.

Process for the Preparation of Losartan

The invention relates to an improved process for the preparation of Losartan. The process comprising reacting 2-n-butyl-4-chloro-5-formyl imidazole with 2-(4-bromomethyl) benzonitrile in the presence of a phase transfer catalyst and an alkali, and reducing the resulting cyano aldehyde to produce a cyano alcohol which is further reacted with sodium azide in N-methyl pyrrolidinone and a salt to produce Losartan.

Process for the preparation of losartan

The invention relates to a improved process for the preparation of Losartan and its potassium salt, which comprises: (i) reacting bromo OTBN with BCFI in the presence of a base and a phase transfer catalyst to produce a cyano aldehyde; reacting the formed cyano aldehyde with sodium azide in the presence of tributyl tin chloride to produce aldehyde tetrazole; reducing the formed aldehyde tetrazole with sodium borohydride to produce Losartan; and, if desired, converting the formed Losartan to its potassium salt by known method.

A process for the preparation of sartan derivates and intermediates useful in such process

The invention provides a process for the preparation of a sartan derivative of formula (I) wherein the substituents have the meaning indicated in the description, or a pharmaceutically acceptable salt thereof, comprising reacting 2-cyanophenylboronic acid or a derivative thereof with a p-halobenzyl-1H-imidazole derivative of formula (VI), wherein , X, Y, R1 and R2 are as defined above, and Z is I, Br or Cl, in the presence of a transition metal catalyst and an inorganic or organic base. The invention also provides new intermediates of formula (V), wherein M is an alkali metal or an NR4R5R6R7 group; and of formula (II)

PROCESS FOR THE PREPARATION OF LOSARTAN

The invention relates to a improved process for the preparation of Losartan and its potassium salt, which comprises (i) reacting bromo OTBN with BCFI in the presence of a base and a phase transfer catalyst to get cyano aldehyde, reacting the cyano aldehyde sodium azide in the presence of tributyl tin chloride to form aldehyde tetrazole , reducing the aldehyde tetrazole with sodium borohydride to give Losartan and , if desired , converting it to its potassium salt by known method .

AN IMPROVED PROCESS FOR THE PREPARATION OF LOSARTAN

The invention relates to an improved process for the preparation of Losartan. Which comprises reacting 2-n-butyl-4-chloro-5-formyl imidazole with 2-(4-bromomethyl) benzonitrile in the presence of a phase transfer catalyst and alkali, and reducing resulting cyano aldehyde to get cyano alcohol which is further reacted with sodium azide in N-methyl pyrrolidinone and a salt to produce Losartan .