3335-44-2Relevant articles and documents
Simple and highly efficient method for the deprotection of allyl ethers using dimethylsulfoxide-sodium iodide
Nagaraju,Krishnaiah,Mereyala, Hari Babu
, p. 2467 - 2472 (2007)
A simple and highly efficient method for deprotection of allyl ethers has been developed using dimethylsulfoxide-sodium iodide (catalytic amount). This method is inexpensive, has simple reaction conditions, has an easy workup procedure, proceduces excellent yields (60-99%), and is effective for several structurally varied allyl ethers. Copyright Taylor & Francis Group, LLC.
Green Synthetic Approach and Antimicrobial Evaluation for Some Novel Pyridyl Benzoate Derivatives
Eldeab
, p. 1034 - 1040 (2019/09/06)
Two series of substituted pyridyl 4-chlorobenzoates have been synthesized by microwave-assisted condensation of the corresponding 2-oxo-1,2-dihydropyridine-3-carbonitriles with 4-chlorobenzoyl chloride under solvent-free conditions. Alternatively, some compounds have also been prepared by conventional heating in methylene chloride in the presence of triethylamine. The structure of the synthesized compounds has been confirmed by spectral data (FTIR, 1D and 2D NMR). The new pyridyl benzoates were evaluated for antibacterial activity against gram-negative and gram-positive bacteria. The activity of 3-cyano-5-[(4-hydroxyphenyl)diazenyl]-4-methyl-6-phenylpyridin-2-yl 4-chlorobenzoate against gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) was comparable to that of amikacin used as standard antibiotic.
Synthesis and adenosine receptors binding studies of new fluorinated analogues of pyrido[2,3-d]pyrimidines and quinazolines
Chandrasekaran, Balakumar,Deb, Pran Kishore,Kachler, Sonja,Akkinepalli, Raghuram Rao,Mailavaram, Raghuprasad,Klotz, Karl-Norbert
, p. 756 - 767 (2017/11/03)
A series of new fluorine containing pyrido[2,3-d]pyrimidines and imidazo[1,2-c]pyrido[3,2-e]pyrimidines along with a series of bioisosteric fluorinated quinazolines were synthesised following appropriate synthetic schemes and characterised by spectral analytical means. X-ray crystal structure of the key precursor 1 (2-amino-3-cyano-4-trifluoro-methyl-6-phenyl-pyridine) was also determined to gain insight into its reactivity. Binding affinity data of all the compounds for adenosine receptors (ARs) showed that pyrido[2,3-d]pyrimidine scaffold with free amino (NH2) group at 2- and 4-position (2a) exhibited the maximum binding affinity for hA3 AR with similar affinity for the hA1 and somewhat lower affinity for hA2A ARs resulting in a compound with no A3 selectivity vs. A1 and moderate selectivity vs. A2A AR (Ki hA1 = 0.62 μM, hA2A = 3.59 μM and hA3 = 0.42 μM). Interestingly, the replacement of both the amino groups with carbonyl (C=O) groups (compound 4) resulted in significantly improved affinity for hA1 AR but with moderate selectivity against hA2A and hA3 ARs (Ki hA1 = 0.17 μM, hA2A = 0.67 μM and hA3 =0.68 μM). In case of fluorinated quinazolines, only compound 18a showed remarkable affinity for hA1 AR with significant selectivity against hA2A and hA3 ARs (Ki hA1 = 0.73 μM, hA2A CloseSPigtSPi 30 μM and hA3 = 9.27 μM). The preliminary results of these compounds demonstrate that the fluorinated pyrido[2,3-d]pyrimidine and imidazo[1,2-c]pyrido[3,2-e]pyrimidine can be considered as promising scaffolds for further optimisation in search of potential antagonists with better affinity and selectivity towards hA1 and hA3 ARs.
