41498-10-6Relevant articles and documents
Cu(I)-promoted one-pot click-SNAr reaction of nitrobenzaldehydes
Su, Changhui,Ding, Zhiyuan,Liu, Xia,Cui, Kai,Ma, Jiejie
supporting information, p. 1068 - 1073 (2016/07/16)
A series of 1,4-disubstituted 1,2,3-triazoles containing formyl was synthesized from a variety of readily available nitrobenzaldehydes and alkynes via a convenient one-pot, click-SNAr reaction with moderate to excellent yields. The reactions we
Facile one-pot synthesis of monosubstituted 1-aryl-1h-1,2,3-triazoles from arylboronic acids and prop-2-ynoic acid (=propiolic acid) or calcium acetylide (=calcium carbide) as acetylene source
Yang, Qing,Jiang, Yubo,Kuang, Chunxiang
experimental part, p. 448 - 454 (2012/05/04)
The synthesis of monosubstituted 1-aryl-1H-1,2,3-triazoles was achieved in a one-pot reaction from arylboronic acids and prop-2-ynoic acid or calcium acetylide (=calcium carbide), respectively, as a source of acetylene, with yields ranging from moderate to excellent (Scheme 1, Table 2). The reaction conditions were successfully applied to arylboronic acids, including analogs with various functionalities. Unexpectedly, the 1,2,3-triazole moiety promoted a regioselective hydrodebromination (Scheme 2). Copyright
Inhibitors of acyl-coA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N- (heteroaryl-substituted benzyl)-N'-arylureas
Tanaka, Akira,Terasawa, Takeshi,Hagihara, Hiroyuki,Sakuma, Yuri,Ishibe, Noriko,Sawada, Masae,Takasugi, Hisashi,Tanaka, Hirokazu
, p. 2390 - 2410 (2007/10/03)
A series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylurea and related derivatives represented by 2 and 3 have been prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyltransferase in vitro and to lower plasma cholesterol levels in cholesterol-fed rats in vivo. Among these novel compounds, the type 3 series was superior. A pyrazol-3-yl group on the N-benzyl group of this trisubstituted urea (i.e. 3, Ar1 = pyrazol-3- yl) was identified as a heteroaromatic ring providing a good profile of biological activity. As a result of optimization of the combination with the N-alkyl group (R) and N-aryl group (At3), compound 3aq (FR186054) was identified as a new, orally efficacious ACAT inhibitor, which exhibited potent in vitro ACAT inhibitory activity (rabbit intestinal microsomes IC50 = 99 nM) and excellent hypocholesterolemic effects in cholesterol-fed rats, irrespective of administration mode (ED50 = 0.046 mg/kg dosed via the diet, ED50 = 0.44 mg/kg administered by gavage in PEG400 vehicle). Moreover, a toxicological study revealed compound 3aq to be nontoxic to the adrenal glands of dogs when tested at a single dose of 10 mg/kg po.