136834-58-7Relevant academic research and scientific papers
Synthesis and biological evaluation of novel potent angiotensin II receptor antagonists with anti-hypertension effect
Nie, Yong-Yan,Da, Ya-Jing,Zheng, Hao,Yang, Xiao-Xia,Jia, Lin,Wen, Cai-Hong,Liang, Li-Sha,Tian, Juan,Chen, Zhi-Long
experimental part, p. 2747 - 2761 (2012/05/20)
A series of novel angiotensin II type 1 receptor antagonists were prepared. Radioligand binding assay suggested that compounds 1b and 1c could be recognized by the AT1 receptor with an IC50 value of 1.6 ± 0.09 nM and 2.64 ± 0.7 nM, respectively. In vivo anti-hypertension experiments showed that compounds (1a, 1b, 1c, 1e) elicited a significant decrease in SBP and DBP of spontaneous hypertensive rats (SHRs). The antihypertensive effects maintained for 10 h, which indicated that these compounds had a favorable blood pressure-lowering effect. Acute toxicity testing suggested that the LD50 value of compound 1b was 2316.8 mg/kg which was lower than valsartan (LD50 = 307.50 mg/kg) but higher than losartan (LD50 = 2248 mg/kg). So they could be considered as novel anti-hypertension candidates and deserved for further investigation.
Pinacolborane as the boron source in nitrogen-directed borylations of aromatic N, N -dimethylhydrazones
López-Rodríguez, Rocío,Ros, Abel,Fernández, Rosario,Lassaletta, José M.
, p. 9915 - 9920 (2013/01/15)
A mild procedure for the Ir(III)-catalyzed nitrogen-directed ortho borylation of aromatic N,N-dialkylhydrazones using pinacolborane as the boron source has been developed. The methodology relies on a modified, hemilabile N,N ligand built on a 4-N,N-dimethylaminopyridine unit that provides high reactivity while maintaining exclusive ortho-selectivity. This procedure can be combined with Suzuki-Miyaura cross-couplings in a 'one-pot' fashion to afford functionalized biaryl derivatives that, upon subsequent 'one-pot', high yielding transformations, provide a convenient entry for the preparation of advanced benzonitrile intermediates for the synthesis of Sartan-type drugs.
Copper-catalyzed synthesis of phenanthridine derivatives under an oxygen atmosphere starting from biaryl-2-carbonitriles and grignard reagents
Zhang, Line,Ang, Gim Yean,Chiba, Shunsuke
supporting information; experimental part, p. 3682 - 3685 (2010/10/20)
A copper-catalyzed synthesis of phenanthridine derivatives was developed starting from biaryl-2-carbonitriles and Grignard reagents. The present transformation is carried out by a sequence of nucleophilic addition of Grignard reagents to biaryl-2-carbonitriles to form N-H imines and their Cu-catalyzed C-N bond formation on the aromatic C-H bond, where molecular oxygen is a prerequisite to achieve the catalytic process.
