42899-64-9Relevant articles and documents
Synthesis of β-ketonitriles, α,β-alkynones and biscabinols from esters using tert-butoxide-assisted C(=O)-C (i.e., acyl-C) coupling under ambient conditions
Kim, Bo Ram,Lee, Hyung-Geun,Kang, Seung-Beom,Jung, Kwang-Ju,Sung, Gi Hyeon,Kim, Jeum-Jong,Lee, Sang-Gyeong,Yoon, Yong-Jin
, p. 10331 - 10336 (2013/11/19)
We demonstrated the synthesis of β-ketonitriles, α,β- alkynones, and biscarbinols using tert-butoxide-assisted C(CO)-C (i.e., acyl-C) coupling of esters under ambient conditions. tert-Butoxide-assisted C(CO)-C (i.e., acyl-C) coupling of esters with cyanomethylenes and acetylenes under transition metal-free ambient conditions gives β-ketonitriles, α,β-alkynones and/or aryl bis(phenylethynyl)carbinols in moderate-to-good yields. It is noteworthy that this is a rapid, facile, and efficient process under ambient conditions, and use of cheap and stable starting materials.
Substituted (1,2-Diarylethyl)amide Acyl-CoA:Cholesterol Acyltransferase Inhibitors: Effect of Polar Groups on in Vitro and in Vivo Activity
Clader, John W.,Berger, Joel G.,Burrier, Robert E.,Davis, Harry R.,Domalski, Martin,et al.
, p. 1600 - 1607 (2007/10/02)
Substituted (1,2-diarylethyl)amides have been prepared and evaluated for their ability to inhibit microsomal acyl-CoA:cholesterol acyltransferase activity in vitro and to lower hepatic cholesteryl ester content in vivo in a cholesterol-fed hamster.Simple unsubstituted (diarylethyl)amides were potent inhibitors in vitro but showed poor activity in vivo.Introduction of polar groups at specific locations on the diarylethylamine moiety decreased in vitro activity but increased in vivo activity.Both effects were highly structure dependent, suggesting specific interactions which were mediating activity in each model.Optimization of these opposing effects led to compounds which were potent in both models.
