329329-57-9Relevant academic research and scientific papers
Efficient synthesis of N-allylated 2-nitroiminoimidazolidine analogues from Baylis–Hillman bromides
Kumar, Sriramoju Bharath,Pavan Kumar, Chebolu Naga Sesha Sai,Santhoshi, Amlipur,Kumar, Koochana Pranay,Murthy,Jayathirtha Rao, Vaidya
, p. 131 - 136 (2017)
Various Baylis–Hillman–derived new N-allylated 2-nitroiminoimidazolidine analogs were efficiently prepared using potassium carbonate as base. Simple workup procedure, excellent yields, and mild reaction conditions are the salient features of this method. All the synthesized compounds are screened for their larvicidal activity on fourth instar mosquito larvae, Culex quinquefasciatus.
Synthesis of 1-benzhydryl piperazine derivatives and evaluation of their ACE inhibition and antimicrobial activities
Santhoshi, Amlipur,Kumar, Singam Naveen,Sujitha, Pombala,Poornachandra, Yedla,Sadhu, Partha Sarathi,Kumar, C. Ganesh,Rao, Vaidya Jayathirtha
, p. 3207 - 3219 (2014/05/06)
This study presents the synthesis of 14 new 1,4-disubstituted piperazine derivatives from allyl bromides of Baylis-Hillman adduct and 4,4-disubstituted benzhydryl piperazines. All the synthesized compounds were further screened for in vitro ACE inhibitor and antimicrobial activities. Among the synthesized piperazine derivatives, compound 12h showed moderate ACE inhibitor activity as compared to the standard, angiotensin-converting enzyme inhibitor (Sigma). The kinetic data (K m, K i and V max values) of enzyme inhibition for compound 12h and ACE inhibitor standard were also determined. Similarly, all compounds were screened against different bacterial strains. Compounds 12a, 12b, 12d, 12h and 12i showed excellent to moderate activity against various tested bacterial strains. Compounds 12b and 12i showed broad spectrum of antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, S. aureus MLS 16, Escherichia coli, Bacillus subtilis and Klebsiella planticola, while compounds 12a, 12d and 12i showed promising activity against P. aeruginosa (MIC value of 8.96 μM), S. aureus (MIC value of 42.2 μM) and S. aureus MLS 16 (MIC value of 81.3 μM), respectively. The remaining compounds showed activity at a concentration of >491 μM.
Expedient synthesis of β,β-disubstituted α- methylenepropionates
Biswas, Kallolmay,B?rner, Christoph,Gimeno, Josepe,Goldsmith, Paul J.,Ramazzotti, Daniella,So, Angela L.K.,Woodward, Simon
, p. 1433 - 1442 (2007/10/03)
Baylis-Hillman alcohols are excellent sources of the allylic halides ArCHCH(CH2X)(CO2R) (X=Br, Cl; R1=Me, Et, But). The Z double bond isomers are attained in high isomeric purity (>14:1, Z/E). The halides are ch
Asymmetric chemo- and regiospecific addition of organozinc reagents to Baylis-Hillman derived allylic electrophiles
Borner,Gimeno,Gladiali,Goldsmith,Ramazzotti,Woodward
, p. 2433 - 2434 (2007/10/03)
The copper-catalysed S(N)2' addition of ZnR2 to allylic (Z)-ArCH=C(CH2X)(CO2Et) (X = Br, Cl, OSO2Me) fashions only ArCH(R)C(=CH2)(CO2Et); use of a chiral ligand gives up to 64% ee for this
