114772-54-2Relevant articles and documents
An efficient, commercially viable, and safe process for preparation of losartan potassium, an angiotensin II receptor antagonist
Madasu, Suri Babu,Vekariya,Koteswaramma, Ch,Islam, Aminul,Sanasi, Paul Douglas,Korupolu, Raghu Babu
, p. 2025 - 2030 (2012)
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.
Bacterial Peptide deformylase inhibition of cyano substituted biaryl analogs: Synthesis, in vitro biological evaluation, molecular docking study and in silico ADME prediction
Khan, Firoz A. Kalam,Patil, Rajendra H.,Shinde, Devanand B.,Sangshetti, Jaiprakash N.
, p. 3456 - 3463 (2016)
Herein, we report the synthesis and screening of cyano substituted biaryl analogs 5(a–m) as Peptide deformylase (PDF) enzyme inhibitors. The compounds 5a (IC50value?=?13.16?μM), 5d (IC50value?=?15.66?μM) and 5j (IC50value?=?19.16?μM) had shown good PDF inhibition activity. The compounds 5a (MIC range?=?11.00–15.83?μg/mL), 5b (MIC range?=?23.75–28.50?μg/mL) and 5j (MIC range?=?7.66–16.91?μg/mL) had also shown potent antibacterial activity when compared with ciprofloxacin (MIC range?=?25–50?μg/mL). Thus, the active derivatives were not only potent PDF inhibitors but also efficient antibacterial agents. In order to gain more insight on the binding mode of the compounds with PDF, the synthesized compounds 5(a–m) were docked against PDF enzyme of Escherichia coli and compounds exhibited good binding properties. In silico ADME properties of synthesized compounds were also analyzed and showed potential to develop as good oral drug candidates.
Readily Reconfigurable Continuous-Stirred Tank Photochemical Reactor Platform
Blacker, A. John,Francis, Daniel,Kapur, Nikil,Marsden, Stephen P.
supporting information, (2022/01/12)
A new modular photochemical continuous stirred-tank reactor (CSTR) design is described, based upon the development of light-source units that can be fitted to the previously described fReactor CSTR platform. In addition to use in homogeneous photochemical reactions (e.g., photoredox-catalyzed hydroamination), these units are especially well suited to handling multiphasic mixtures, exemplified here in solid-liquid (Wohl-Ziegler bromination) and gas-liquid (photocatalytic oxidative decarboxylation) reactions. The use of slurries as input feeds allows for the intensification of photochemical brominations, while the modular nature of the system facilitates the simple integration of downstream reaction steps, exemplified here in a continuous synthesis of an intermediate for the antihypertensive drug valsartan.
Preparation method of normal-temperature bromoethyl cyanobiphenyl based on dibromohydantoin
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Paragraph 0037-0057, (2020/07/13)
The invention discloses a preparation method of normal-temperature bromoethyl cyanobiphenyl based on dibromohydantoin, and belongs to the technical field of pharmaceutical chemicals, and particularlydiscloses a method for preparing substituent-containing bromoethyl cyanobiphenyl by using a flowing photochemical method. According to the method, an oxidant and a radical initiator are not needed; methyl biphenyl is used as a raw material, dibromohydantoin is used as a bromination reagent, acetone, dichloromethane, petroleum ether or acetonitrile is used as a solvent, and after the raw material and the bromination reagent are respectively mixed with the solvent, the mixture flows into a pipeline through an injection pipe, is mixed by a mixer, then enters a constant-temperature water bath reactor and is subjected to a reaction through illumination. The 2-cyano-4 '-bromomethylbiphenyl synthesized by the method is good in purity, high in yield, simple in reaction system and low in toxicity,is suitable for industrial application in the field of biological medicines, can be suitable for an automatic continuous production process, and conforms to the development concepts of green chemicalindustry, high efficiency and economy.
Preparation method of bromo-sartan biphenyl based on hydrogen peroxide-hydrobromic acid system
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Paragraph 0036-0056, (2020/07/15)
The invention discloses a preparation method of bromo-sartan biphenyl based on a hydrogen peroxide-hydrobromic acid system, and belongs to the technical field of pharmaceutical chemicals. The invention discloses a method for preparing substituent-containing bromo-sartan biphenyl by using a flowing photochemical method. According to the method, methyl biphenyl is used as a raw material, hydrobromicacid is used as a bromination reagent, hydrogen peroxide is used as an oxidation reagent, acetonitrile or ethyl acetate is used as a solvent, and after the raw material, the bromination reagent and the oxidation reagent are respectively mixed with the solvent, the mixture flows into a pipeline through an injection pipe, is mixed through a mixer, enters a constant-temperature water bath reactor and undergoes a reaction through illumination. The 2-cyano-4'-bromomethylbiphenyl synthesized by the method is good in purity, high in yield, simple in a reaction system, low in toxicity and high in atom conversion rate, is suitable for industrial application in the field of biological medicines, can be suitable for an automatic continuous production process, and conforms to the development conceptsof green chemical industry, high efficiency and economy.
