114772-55-3Relevant articles and documents
Synthesis and evaluation of novel angiotensin II receptor 1 antagonists as anti-hypertension drugs
Bao, Xiaolu,Zhu, Weibo,Zhang, Ruijing,Wen, Caihong,Wang, Li,Yan, Yijia,Tang, Hesheng,Chen, Zhilong
, p. 2023 - 2031 (2016)
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
Synthesis, characterization and biological evaluation of benzimidazole and benzindazole derivatives as anti-hypertensive agents
Silky, Sethy,Mandal, Sudip Kumar,Ewies, Ewies Fawzy,Neerupma, Dhiman,Arun, Garg
, p. 3659 - 3664 (2021/07/10)
A substituted benzimidazole and benzindazole derivatives had been synthesized having antihypertensive activity through antagonizing the angiotensin II (Ang II) receptors. The in vivo antihypertensive activity of the compounds was done with acute renal hypertension model. Two compounds TG 1 and TG 3 were found to have antihypertensive activity comparable to Telmisartan which is a prototype for Angiotensin II receptor antagonists class of drugs.In an antihypertensive study the compounds TG 1, TG 2 and TG 3 had systolic blood pressures of 147.2 mm/Hg, 168.2 mm/Hg, and 126.3 mm/Hg, respectively. This systolic blood pressure was lower than the disease control vehicle-treated rodents, which had a systolic blood pressure of 167.2 mm/Hg. The diastolic blood pressure was 119.7 mm/Hg, 124.7 mm/Hg and 88.83 mm/Hg, respectively and that of the disease control vehicle-treated rodents was 122.3 mm/Hg. TG 3 had comparable decrease in the MABP to Telmisartan. These encouraging results make compound TG 3 effective anti-hypertensive drug candidate and worthy of further investigation.
Process for catalytic synthesis of 2-cyano-4'-methyl biphenyl
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Paragraph 0018-0088, (2021/04/17)
The invention relates to a method for catalytic synthesis of 2-cyano-4'-methyl biphenyl. The process comprises the following steps: firstly, preparing a phosphine-containing material carrier: putting a phosphine ligand, triphenyl benzene and dimethoxy methane into a reaction kettle in proportion, then adding phosphotungstic acid, and preparing a phosphine-containing polymer carrier at a high temperature under protective gas; then, performing catalytic synthesis to obtain 2-cyano-4'-methyl biphenyl: adding a carrier, metal palladium and an o-chloro benzonitrile substrate, adding p-toluene boronic acid, adding a solvent, adding alkali, and obtaining 2-cyano-4'-methyl biphenyl at medium-high temperature and under reaction pressure. The method has the advantages that the catalyst can be recycled and has higher activity and selectivity and good stability, the loss of metal palladium is prevented, and the method is suitable for industrial production.
[Pd(4-R3Si-IPr)(allyl)Cl]/K2CO3/EtOH: A highly effective catalytic system for the Suzuki-Miyaura cross-coupling reaction
Choe, Yoong-Kee,Choi, Jun-Chul,Faried, Miftah,Fukaya, Norihisa,Lee, Vladimir Ya.,Matsumoto, Kazuhiro,Mizusaki, Tomoteru,Putro, Wahyu S.,Seo, Yuto,Takagi, Yukio
, (2021/10/05)
A series of R3Si-NHC-Pd complexes 1Pd-7Pd was successfully tested as a pre-catalyst for the Suzuki-Miyaura cross-coupling reaction of aryl chlorides and arylboronic acid derivatives to form a wide range of valuable biphenyl products. Use of the readily available weakly basic potassium carbonate as a base and the highly polar protic ethanol as the reaction solvent gave the target coupling products in good-to-excellent yields. The experimental data pointed to the crucial importance of the preliminary pre-catalyst activation step [i.e., the conversion of Pd(II) to Pd(0)], which is remarkably facilitated by the electron-donating trialkylsilyl groups on the NHC ligands of 1Pd–7Pd, thereby rendering them superior compared to the commercially available IPr-Pd complexes. Computational analysis revealed the mechanism of the Pd(II)→Pd(0) activation step, demonstrating the critical role of the reaction solvent and the base in the preference of our 1Pd–7Pd pre-catalysts, for which this step is both thermodynamically and kinetically more feasible.
