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.
Photocatalytic continuous bromination method
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Paragraph 0070-0071, (2021/04/03)
The invention provides a photocatalytic continuous bromination method. The method comprises the following steps: carrying out a first-stage photocatalytic continuous bromination reaction on a materialcontaining an aromatic substrate with a structural general formula I and a bromination reagent in a first continuous illumination reactor to form a first continuous system; overflowing the obtained first continuous system into a second continuous illumination reactor for a second-stage photocatalytic continuous bromination reaction to form a second continuous system; and purifying the second continuous system, wherein the structural general formula I is shown in the specification, R is selected from any one of carboxyl, ester group, NO2, CN, C1 to C8 alkyl and alkoxy, and R1 is C1 to C8 alkyl; n is 1 or 2; X is N or C, and the bromination reagent is Nbromo succinimide or dibromohydantoin. According to the bromination reagent, the selectivity of a product is improved, so the yield of the product is improved; the photocatalytic continuous bromination reaction of the two stages effectively relieves the reaction heat accumulation, and enhances the yield of the target product.
Preparation method of bromoilsartan soluble in 1,2 - dichloroethane (by machine translation)
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Paragraph 0036-0054, (2020/07/12)
The invention discloses a preparation method of brominated sartan biphenyl dissolved 1,2 - dichloroethane, and belongs to the technical field of pharmaceutical chemical engineering. The method uses methylbiphenyl as a raw material, 1,2 - dichloroethane as a solvent, and a brominated reagent, dibromohydantoin, N - bromosuccinimide or sodium bromide and sodium bromate. 2 - Cyano -4 ’ - bromomethylbiphenyl synthesized by the method is good in purity, high in yield, simple in reaction system, low in toxicity, high in atom conversion rate and suitable for industrial application in the field of biological medicine. (by machine translation)
High-temperature preparation method of 4'-bromomethyl-2-cyanobiphenyl based on bromine
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Paragraph 0038-0058, (2020/07/12)
The invention discloses a high-temperature preparation method of 4'-bromomethyl-2-cyanobiphenyl based on bromine, belongs to the technical field of pharmaceutical chemicals, and particularly disclosesa method for preparing substituent-containing 4'-bromomethyl-2-cyanobiphenyl by using a flowing photochemical method. An oxidant and a radical initiator are not needed; and methyl biphenyl is used asa raw material, bromine is used as a bromination reagent, ethyl acetate, glacial acetic acid or N,N-dimethylformamide is used as a solvent, and after the raw material and the bromination reagent arerespectively mixed with the solvent, the obtained mixtures flow into a pipeline through injection pipes, and are mixed by a mixer, and then the obtained mixture enters a constant-temperature water bath reactor and is subjected to a reaction through illumination. The 4'-bromomethyl-2-cyanobiphenyl 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 chemical industry, high efficiency and economy.
