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  • Open access
  • 68 Reads
Synthesis of New 1-Substituted-4-(2-phenylquinazolin-4-yl and 4-ylidene)
Two new 1-substituted-4-(2-phenylquinazolin-4-yl and 4-ylidene) thiosemicarbazides 3 and 5 were formed by multistep domino reaction of imidoyl isothiocyanate derivative 1 with 1,1-di-R hydrazine in acetone solution. Applied hydrazine hydrate under the same reaction condition afforded 4-(2-phenylquinazolin-4(3H)-ylidene)-2-(prop-1-en-2-yl)-1- (propan-2-lidene) thiosemicarbazide (7) via six step three component domino reaction. Compounds 3, 5 and 7 were identified by CHNS elemental analysis, 1 H-NMR,13 C-NMR spectral data and their correlation with ones from known structural motives.
  • Open access
  • 83 Reads
Convenient Synthesis of Novel Amino Acid Coupled Benzanilides
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A facile and convenient synthesis of a variety of Methyl 2-(2-Benzoylaminobenzoylamino) alkanoate 4a-d has been developed by the DCC coupling of 2- Benzoylamino-benzoic acid with amino acid methyl ester. Compounds 4a-c were alternatively prepared by the reaction of aminoacid ester with 3,1-benzoxazinone 2 in pyridine. Dipeptides 8a-j were subsequently prepared following the azide coupling method. Compounds 4 and 8 were expected to possess antimicrobial activity.
  • Open access
  • 73 Reads
Different Behaviouof of Disubtituted Aromatic Heterocycles in Polar Diels-Alder Reactions
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Dienophilic behaviour of disubstituted aromatic heterocycles towards normal electron demand Diels-Alder reactions is studied under thermal conditions. Formation of pyrrolyl-thiophenes are observed only in the reactions of nitrothiophenes with isoprene.
  • Open access
  • 62 Reads
Isoprene-mediated lithiation of chiral N-alkylimidazoles
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The isoprene-mediated lithiation of different chiral N-alkylimidazoles (2a and 2b) and the following reaction with pivalaldehyde leads to the corresponding imidazolylpropanol derivatives 4 and 5 with excellent overall yield, but low de (up to 26%).
  • Open access
  • 46 Reads
An Easy Synthesis of 5-Nitro-Thiophenes and 3-Amino-2-Nitro-Thiophenes
A one-step preparation of substituted 5-nitro thiophenes and 3-amino-2-nitrothiophenes starting from corresponding β-chloroacroleins and β-chloropropenonitriles was developed. Sodium sulfide, bromonitromethane and sodium hydroxide were used as reagents to obtain the expected compounds in good yields with a simple and easy work up procedure.
  • Open access
  • 57 Reads
Synthesis and Hydrophobic Properties of New 2-Aryl-5,7-di-tert-butylbenzoxazoles
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The series of fifteen lipophilic 2-aryl-5,7-di-tert-butylbenzoxazoles substituted in the phenyl ring was prepared by the reaction of 2-amino-4,6-di-tert-butylphenol with the appropriated aldehydes. The general synthetic approach of all newly synthesized compounds is presented. All the substituted 5,7-di-tert-butylbenzoxazole derivatives were analyzed using the reversed phase high performance liquid chromatography (RP-HPLC) method for the lipophilicity measurement. The procedure was performed under isocratic conditions with methanol as an organic modifier in the mobile phase using end-capped non-polar C18 stationary RP column. In the present study the correlation between RP-HPLC retention parameter log K (the logarithm of capacity factor K) and log P data calculated in various ways is shown. The relationships between the lipophilicity and the chemical structure of the studied compounds are discussed as well.
  • Open access
  • 50 Reads
Stereoselective synthesis of the advanced precursor of (+)-myriocin
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A stereoselective approach toward 2-amino-1,3-propanediol 13 is described. This compound represents the key intermediate in the total stereoselective synthesis of (+)-myriocin 1, an inhibitor of serine palmitoyltransferase (SPT). Moreover, synthon 13 can be used for synthesis of mycriocin analogues. 2-amino-1,3-propanediol moiety is necessary for their biological activity.