61712-98-9Relevant academic research and scientific papers
Lewis Acid-Mediated Ring-Opening Reactions of trans-2-Aroyl-3-styrylcyclopropane-1,1-dicarboxylates: Access to Cyclopentenes and E,E-1,3-Dienes
Thangamani, Murugesan,Srinivasan, Kannupal
, p. 571 - 577 (2018/01/27)
The ring-opening reaction of trans-2-aroyl-3-styrylcyclopropane-1,1-dicarboxylates was investigated with different Lewis acids. With SnCl4, the cyclopropane dicarboxylates afforded cyclopentene derivatives through ring opening followed by cyclization (vinylcyclopropane-cyclopentene rearrangement). With TiCl4, they furnished E,E-1,3-diene derivatives stereoselectively via ring opening followed by proton elimination.
Synthesis, biological evaluation and QSAR studies of diarylpentanoid analogues as potential nitric oxide inhibitors
Mohd Faudzi,Leong,Abas,Mohd Aluwi,Rullah,Lam,Ahmad,Tham,Shaari,Lajis
, p. 1069 - 1080 (2015/06/25)
A series of forty-five 1,5-diphenylpenta-2,4-dien-1-one analogues were synthesized and evaluated for their nitric oxide (NO) inhibition activity in IFN-γ/LPS-activated RAW 264.7 cells. Compounds 3h, 7a, 7d and 7e exhibited comparable or significantly higher activity than the standard, curcumin (IC50 = 14.69 ± 0.24 μM). Compound 7d, a 5-methylthiophenyl-bearing analogue, displayed the most promising NO-inhibitory activity with an IC50 value of 10.24 ± 0.62 μM. The 2D and 3D QSAR analyses performed revealed that a para-hydroxyl group on ring B and an α,β-unsaturated ketone moiety on the linker are crucial for a remarkable anti-inflammatory activity. Based on ADMET and TOPKAT analyses, compounds 3h, 7a and 7d are predicted to be nonmutagenic and to exhibit high blood-brain barrier (BBB) penetration, which indicates that they are potentially effective drug candidates for treating central nervous system (CNS) related disorders.
Asymmetric direct michael addition of acetophenone to α,β- unsaturated aldehydes
Li, Wenjun,Wu, Wenbin,Yang, Juanjuan,Liang, Xinmiao,Ye, Jinxing
experimental part, p. 1085 - 1091 (2011/05/14)
The asymmetric direct Michael addition of ,-unsaturated aldehydes with acetophenone catalyzed by a Jorgensen-Hayashi-catalyst in methanol was developed and the corresponding Michael products of -keto aldehydes could be afforded in up to 82% yield and 98% ee. Georg Thieme Verlag Stuttgart.
