- METHOD FOR PREPAREING 1,3,4-OXADIAZOL UNDER SOLVENT-FREE CONDITION
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The present invention relates to a synthesis method of 1,3,4-oxadiazol, comprising: 1) under a solvent-free condition and by means of a mechanical pulverization method, making a hydrazide compound react with an aldehyde compound and thereby synthesizing a N-acylhydrazone compound; and 2) under a solvent-free condition, adding an iodine-based oxidizing agent to the N-acylhydrazone compound to synthesize 1,3,4-oxadiazol via oxidative cyclization. The solventless synthesis method of 1,3,4-oxadiazol according to the present invention is easy to perform and handle, and has the advantage of synthesizing 1,3,4-oxadiazol at high selectivity and yield. Also, the solventless synthesis method of the present invention can prevent the formation of side products caused by the minute amount of water that usually remains in solvents, and can further prevent synthesized intermediates from being converted back into the starting materials by the water.COPYRIGHT KIPO 2016
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Paragraph 0069-0073; 0269-0270
(2017/02/24)
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- Synthesis of 4-methoxybenzoylhydrazones and evaluation of their antiglycation activity
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A series of 4-methoxybenzoylhydrazones 1-30 was synthesized and the structures of the synthetic derivatives elucidated by spectroscopic methods. The compounds showed a varying degree of antiglycation activity, with IC50 values ranging between 216.52 and 748.71 M, when compared to a rutin standard (IC50 = 294.46 1.50 M). Compounds 1 (IC50 = 216.52 4.2 M), 3 (IC50 = 289.58 2.64 M), 6 (IC50 = 227.75 0.53 M), 7 (IC50 = 242.53 6.1) and 11 (IC50 = 287.79 1.59) all showed more activity that the standard, and these compounds have the potential to serve as possible leads for drugs to inhibit protein glycation in diabetic patients. A preliminary SAR study was performed.
- Taha, Muhammad,Naz, Humera,Rasheed, Saima,Ismail, Nor Hadiani,Rahman, Aqilah Abd,Yousuf, Sammer,Choudhary, Muhammad Iqbal
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p. 1286 - 1301
(2014/02/14)
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- Phthalides by rhodium-catalyzed ketone hydroacylation
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(Chemical Equation Presented) Phthalides are biologically relevant five-membered lactones found in herbs, fruits, and vegetables. Herein we communicate the first atom-economical approach to phthalides by using enantioselective ketone hydroacylation. In the presence of Rh[(Duanphos)]X (X = NO3, OTf, OMs), various 2-ketobenzaldehydes undergo intramolecular hydroacylation to produce phthalide products in good yields and 92-98% ee's. Our study highlights the key role counterions play in controlling both reactivity and enantioselectivity. A concise asymmetric total synthesis of the celery extract (S)-(-)-3-n-butylphthalide is also presented.
- Phan, Diem H. T.,Kim, Byoungmoo,Dong, Vy M.
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supporting information; experimental part
p. 15608 - 15609
(2010/01/30)
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- Design, synthesis and in vitro antimalarial activity of an acylhydrazone library
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A library of acylhydrazone iron chelators was synthesized and tested for its ability to inhibit the growth of a chloroquine-resistant strain of Plasmodium falciparum. Some of these new compounds are significantly more active than desferrioxamine DFO, the
- Melnyk, Patricia,Leroux, Virginie,Sergheraert, Christian,Grellier, Philippe
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- Synthesis and characterization of iron(III) complexes of salicylaldehyde 4-methoxybenzoyl hydrazone
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Iron(III) complexes of salicylaldehyde 4-methoxybenzoyl hydrazone, (H2smbhon), have been isolated and the reactions of [Fe(smbhon) (Cl) (H2O)]2 with SnCl2 and CH3CN are discussed. These complexes have
- Dey, Kamalendu,Bandyopadhyay, Debasish,Bhattacharya, Prabir Kumar,Chakraborty, Kartick
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p. 107 - 111
(2007/10/03)
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- Synthesis of New Acylhydrazones as Iron-Chelating Compounds
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Fourteen acylhydrazides have been condensed with three aromatic o-hydroxy aldehydes (pyridoxal, salicylaldehyde, and 2-hydroxy-1-naphthaldehyde) to give 42 acylhydrazones, of which 38 are new.These compounds complex iron and have shown varying abilities to promote the movement of iron across biological membranes.Their infrared and nuclear magnetic resonance spectra support the structures assigned to them.
- Edward, John T.,Gauthier, Mario,Chubb, Francis L.,Ponka, Premysl
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p. 538 - 540
(2007/10/02)
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- Salicylaldehyde 4-Methoxybenzoylhydrazone and Diacetylbis(4-methoxybenzoylhydrazone) as Ligands for Tin, Lead and Zirconium
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The synthesis and characterisation of tin(II), tin(IV), organotin(IV), lead(II), organolead(IV), zirconium(IV) and organozirconium(IV) complexes with two new ligands salicylaldehyde 4-methoxybenzoyl hydrazone and diacetylbis(4-methoxybenzoylhydrazone) ab
- Dey, Kamalendu,Ray, Satyabrata,Bhattacharyya, Prabir Kumar,Gangopadhyay, Amitava,Bhasin, Kuldip K.,Verma, Ravindra D.
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p. 809 - 814
(2007/10/02)
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