148527-38-2Relevant articles and documents
Synthesis and evaluation of novel 18F-labeled quinazoline derivatives with low lipophilicity for tumor PET imaging
Chong, Yan,Chang, Jin,Zhao, Wenwen,He, Yong,Li, Yuqiao,Zhang, Huabei,Qi, Chuanmin
, p. 42 - 53 (2018/02/06)
Four novel 18F-labeled quinazoline derivatives with low lipophilicity, [18F]4-(2-fluoroethoxy)-6,7-dimethoxyquinazoline ([18F]I), [18F]4-(3-((4-(2-fluoroethoxy)-7-methoxyquinazolin-6-yl)oxy)propyl)morpholine ([18F]II), [18F]4-(2-fluoroethoxy)-7-methoxy-6-(2-methoxyethoxy)quinazoline ([18F]III), and [18F]4-(2-fluoroethoxy)-6,7-bis(2-methoxyethoxy)quinazoline ([18F]IV), were synthesized via a 2-step radiosynthesis procedure with an overall radiochemical yield of 10% to 38% (without decay correction) and radiochemical purities of >98%. The lipophilicity and stability of labeled compounds were tested in vitro. The log P values of the 4 radiotracers ranged from 0.52 to 1.07. We then performed ELISA to measure their affinities to EGFR-TK; ELISA assay results indicated that each inhibitor was specifically bounded to EGFR-TK in a dose-dependent manner. The EGFR-TK autophosphorylation IC50 values of [18F]I, [18F]II, [18F]III, and [18F]IV were 7.732, 0.4698, 0.1174, and 0.1176?μM, respectively. All labeled compounds were evaluated via cellular uptake and blocking studies in HepG2 cell lines in vitro. Cellular uptake and blocking experiment results indicated that [18F]I and [18F]III had excellent cellular uptake at 120-minute postinjection in HepG2 carcinoma cells (51.80?±?3.42%ID/mg protein and 27.31?±?1.94%ID/mg protein, respectively). Additionally, biodistribution experiments in S180 tumor-bearing mice in vivo indicated that [18F]I had a very fast clearance in blood and a relatively high uptake ratio of tumor to blood (4.76) and tumor to muscle (1.82) at 60-minute postinjection. [18F]III had a quick clearance in plasma, and its highest uptake ratio of tumor to muscle was 2.55 at 15-minute postinjection. These experimental results and experiences were valuable for the further exploration of novel radiotracers of quinazoline derivatives.
Polymer supported Zn-salen complexes: An effective one-pot oxidative esterification of aldehydes to carboxylic esters
Balinge, Kamlesh Rudreshwar,Khiratkar, Avinash Ganesh,Bhagat, Pundlik Rambhau
, p. 1085 - 1095 (2017/08/08)
Polymer-supported Zn-salen (PS-Zn-salen) complexes were synthesized, characterized and used as a catalyst for one-pot oxidative esterification of aldehydes with alcohols. The PS-Zn-salen heterogeneous catalyst exhibited a high-performance for the oxidative esterification of aldehydes to the corresponding methyl/ethyl esters using hydrogen peroxide as a green oxidant. Due to the synergistic effect of polymer support, the heterogeneous catalyst presented superior catalytic activity and afford 100% conversion of 3,4,5-trimethoxybenzaldehyde and 4-chlorobenzaldehyde to corresponding esters under optimized conditions. The different alcohol substrates study (viz. methyl alcohol, ethyl alcohol, allyl alcohol and benzyl alcohol) showed reasonable selectivity for esters, indicating the scope of the catalysts. Significantly, the synthesized complexes possess good hydrophobic/heterogeneous properties, which permit facile reclamation of the catalyst by using mere filtration. Moreover, the effect of counter anions of complex also studied which indicated that there is no appreciable influence on the conversion of product. The catalyst was reused up to 5th successive run with the average conversion of ester 87.4%. Mechanistic studies have recognized that this “one pot” direct oxidative esterification proceeds through acid formation, proven by a GC–MS. The catalyst is also found to be very stable, up to 280?°C, confirmed by the thermo gravimetric study.
TETRAZOLE COMPOUNDS FOR REDUCING URIC ACID
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Paragraph 0108, (2015/11/30)
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including g