ALUMINA CATALYST: SYNTHESIS OF NOVEL QUINAZOLINE DE RIVATIVES AND THEIR SOLUBILITY INCREASES THROUGH INCLUSION WITH β-CYCLO DEXTRIN
- Vol.11(2)
- M P Innovare Academic Sciences Pvt Ltd 2019
- 51-58p.
Objective: To synthesis a novel methodology of bioactive quina zoline derivatives under greener process to an exce llent yields and increases their solubility via inclusion with β-cyclodextrin (CD). Methods: Derivatives of quinazoline compounds were prepared by the mixture of 3-amino-2-phenylquinazolin-4(3H)- one, derived from 2-phenyl- 4H-benzo[1,3]oxazin-4-one by refluxing with hydrazi ne, substituted aromatic aldehyde and alumina intim ately in an agate mortar and pestle under solvent-free condition. Using various techniques fo r preparing inclusion complexes, kneaded method is the best method for encapsulation in host- guest complex chemistry. All compounds including in clusion complexes were characterised by spectral me thods. Results: Synthesized a series of novel quinazoline compounds under a very easier greener process with a commerc ially available reagent. However, their low bioavailability, due to low absorption an d solubility, can limit their potential application s. CD was used to resolve this solubility problem. CD can easily accommodated the guest molecules to e ncapsulate inside its cavity due to interior the hy drophobic nature with a hydrophilic exterior part to form thermodynamically more stable molecula r microcapsules, commonly name as host-guest comple xes or inclusion complexes. In this sense, CD was utilized to enhance not only the solu bility and bioavailability of these quinazoline com pounds but also their antibacterial capacity. The formation of inclusion complex was thus confirm ed by ultraviolet-visible spectroscopy (UV-VIS), Fo urier Transform Infrared Spectrometry (FT- IR), differential scanning calorimetry (DSC) and so lubility study technique. Conclusion: Here we have successfully unfolded an eco-friendly methodology for the synthesis of derivatives of qui nazoline and increased their solubility via host-guest inclusion technique. From the spectral analysis, it was concluded that the q uinazoline compound is fully encapsulated inside the cavity of the CD.