2998-04-1Relevant articles and documents
Benzocyclopentanone derivative, and preparation method and application thereof
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Paragraph 0063; 0064, (2019/11/20)
The invention discloses a benzocyclopentanone derivative, a preparation method thereof, and an application of the derivative in inhibition of aflatoxin. The preparation method is characterized in that1,2-phenylenediacetic acid undergoes a series of reactions such as esterification, condensation. nucleophilic substitution, catalytic decarboxylation, Michael addition and high-temperature decarboxylation to finally prepare the benzocyclopentanone derivative. The benzocyclopentanone derivative can inhibit aflatoxin and inhibit the growth of Aspergillus flavus in grains, foods and beverages, and has the advantages of good inhibition effect on the growth and toxin production of Aspergillus flavus, safety, no toxic or side effects, easiness in use, and easiness in industrial production, so the benzocyclopentanone derivative has extremely broad application prospects.
An enantioselective total synthesis of (-)-isoschizogamine
Xu, Zhengren,Bao, Xu,Wang, Qian,Zhu, Jieping
supporting information, p. 14937 - 14940 (2016/02/05)
A concise enantioselective total synthesis of (-)-isoschizogamine, a complex bridged polycyclic monoterpene indole alkaloid, was accomplished. N-Alkylation of an enantio-enriched imine with an alkyl iodide afforded an iminium salt, which, upon heating by microwave irradiation in the presence of pivalic acid, was converted into the hexacyclic structure of natural product by a complex but ordered domino sequence. The one-pot process leading to the formation of one C-C bond and three C-N bonds created three rings and three contiguous stereogenic centers with complete control of both the relative and absolute stereochemistry. Mix and go: Simply heating the alkyl iodide 1 and imine 2 afforded the hexacyclic compound 3, which was subsequently converted, in one step, into (-)-isoschizogamine. Pivalic acid is the only reagent needed to promote this complex yet ordered domino sequence creating three rings and three contiguous stereogenic centers with complete control of both the relative and absolute stereochemistry.
Biodegradable cross-linked poly(amino alcohol esters) based on LMW PEI for gene delivery
Li, Shuo,Wang, Yu,Zhang, Ji,Yang, Wei-Han,Dai, Zhen-Hua,Zhu, Wen,Yu, Xiao-Qi
experimental part, p. 1254 - 1262 (2012/03/10)
Polyethylenimine (PEI, especially with Mw of 25000) has been known as an efficient gene carrier and a gold standard of gene transfection due to its high transfection efficiency (TE). However, high concomitant cytotoxicity limited the application of PEI. In this report, several cationic polymers derived from low molecular weight (LMW) PEI (Mw 600) linked with diglycidyl adipate (DA-PEI) or its analogs (diglycidyl succinate, DS-PEI and diglycidyl oxalate, DO-PEI; D-PEIs for all 3 polymers) were prepared and characterized. GPC gave Mws of DA-PEI, DS-PEI and DO-PEI as 6861, 16015 and 35281, respectively. Moreover, degradation of the ester-containing DS-PEI was also confirmed by GPC. In addition, hydroxyls in these polymers could improve their water solubility. These polymers exhibited good ability to condense plasmid DNA into nanoparticles with the size of 120-250 nm. ζ-potentials of the polyplexes were found to be around +10-20 mV under weight ratios (polymer/DNA) from 0.5 to 32. Agarose gel retardation showed that DNA could be released from the polyplexes after being pre-incubated for 30 h. In vitro experiments were carried out and it was found that DS-PEI showed about 5 times of TE compared to that of the PEI/DNA polyplex under a weight ratio of 1 in A549 cells. Meanwhile, the cytotoxicity of D-PEIs assayed by MTT is lower than that of 25 kDa PEI in HEK293 cells. These results suggested that this series of PEI derivatives would be promising non-viral biodegradable vectors for gene delivery. The Royal Society of Chemistry.