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Piperidine-4-ones, Synthesis of derivatives, biological activities

(Ed.): "Further Components Carboxylic Acid and Amine (Ugi Reaction)", Georg Thieme Verlag KG, Stuttgart, Science of Synthesis: Multicomponent Reactions 1 (2013), pp 415–502.

Synthesized compounds have been evaluated for antibacterial activity at concentration of 50 μg/ml and 100 μg/ml by standard method, against following bacteria:

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The compound 3-amino-2-mercaptoquinazolin-4(3H)-one (2) was synthesized by adding carbondisulphide (1.6 m1. 0.026 mol) and aqueous sodium hydroxide (1.2 m1, 20M) dropwise to a vigorously stirred solution of anthranilic acid (1, 0.02 mol) in dimethylsulfoxide (10 ml) at room temperature. After thirty min dimethylsulphate (2.5g. 0.02 mol) was added dropwisc under cooling with an ice bath. Stirring was continued for 3h, the reaction mixture was then poured into icc water and extracted with chloroform. The solvent was removed by distillation under reduced pressure. Thus the obtained methyl-N-(2-carboxyphenyl) dithiocarbamate was used for further reaction without purification. Hydrazine hydrate (8.6g. 0.2 mol. 80%) was added dropwise with stirring to methyl-N-(2-carhoxyphenyl) dithiocarhamate in cold condition. After completc addition, stirring was continued for 1½ hr at 500C and then it was poured into ice water, the solid obtained was filtered, washed with water dried and recrystallized from dimethylformamide-ethanol mixture to yield (2) as a white crystalline product.

(Eds.): "Enzymatic C-Alkylation of Aromatic Compounds", Georg Thieme Verlag KG, Stuttgart, Science of Synthesis, Biocatalysis in Organic Synthesis 2 (2014), pp 177–211

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The synthesized compounds are screened against bacterias like staphylococcus aureus (Gram +ve) and Escherichia coli (Gram -ve) and Bacillus subtillis (Gram +ve) and Pseudomonas aureus (Gram -ve) and fungi like Candida albicans and Aspergillus flavus to know their antimicrobial activity (by cup plate method).

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CONCLUSION: As shown in the present review, a wide variety of synthetic strategies are being used for the preparation of pharmaceutically active piperidones with a range of potential applications. Due to the demand for improved selectivity and reduction of side effect of drugs in pharmaceutical research are to be designed even in the future.

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Synthesis of Carbamoyl Azides from Primary Amines …


Science of Synthesis: Best methods. Best results – …

He has published over 350 papers on his work in the fields of cell cycle, gene therapy and the genetics of cancer. Giordano has been named a Knight of the Republic of Italy for outstanding achievements in cancer research. In September of 2009, Giordano received the Philip Mazzei "The Bridge" Award from The American University of Rome for his scientific and economic contributions to the United States and Italy. In the past three years, Dr. Giordano's work has been profiled in Philadelphia Magazine, Philadelphia Business Journal, and Science.

Controlling the Synthesis of CoO Nanocrystals with …

Intra molecular Processes: The intramolecular Mannich reaction is a powerful tool for the rapid, efficient, highly stereo selective assembly of polysubstitued piperidones. Sulfinyl amines served as asymmetric precursors to δ-amino-β ketoesters44. Treatement with excess trifluroacetic acid removed the sulfinyl group and the released chiral amine salt was then reacted with an aldehyde or ketone giving polysubstitued piperidone. The Major isomer shown to have the C-2 and C-6 substituents in a cis –orientation with the C-2 and C-3 substituents trans. For aldehydes, nearly exclusive formation of the 2,6-cis-disubstitued piperidone was consistent with transition state. Decarboxylation was effected with 48% HBr in methanol. Some erosion of chirality was noted and was attributed to a retro-Mannich reaction. Disubstitued -4-piperidones serve as an important buiding block for piperidine alkaloid synthesis.

Domino Reactions in the Synthesis of Heterocyclic …

Stereoselective synthesis of piperidine-4-ones: Reviews updating progress in the stereo selective synthesis of substituted piperidines have appeared recently 41. 2,3 –dihydro-4-pyridones were utilized in the synthesis of numerous alkaloids due to the variety of stereo controlled functionalizations that were possible 42. 2-substitued –N-acyl-2,3dihydro-4-pyridones were prepared in an enantiomerically pure state by the stereoselctive addition of organomettailc reagents and metallenolates to chiral 1acylpyridinium salts 43.

Domino reactions in the synthesis of heterocyclic ..

Synthesized compounds of 2,2'-bis-7 substituted-[1,3,4]-thiadiazolo-[2-3-b] quinazolin-5-ones have been evaluated for anti-inflammatory activity (in-vitro). Some of compounds promisingly inhibit albumin denaturation in comparison with standard drugs, ibuprofen exhibited 74.63% inhibition of albumn denaturation.

Quinoxaline as a potent heterocyclic moiety IOSR Journal Of Pharmacy

From this it is concluded that the synthesiled compounds have shown better activity agtainst Aspergillius flavus than Candida albicans.

The Journal of Organic Synthesis of 1-Methylcyclopropene.

Dr. Dang has written more than 200 scientific papers. He is senior editor of Cancer Research and serves on the editorial boards of eight other scientific publications, including the Journal of Molecular Medicine, Current Cancer Therapy Reviews, Drug Discovery Today: Disease Mechanisms, Journal of Clinical Investigations, Neoplasia, Clinical and Translational Science and The Vietnamese Medical Journal. Elected to the National Academy of Sciences' Institute of Medicine in 2006, Dr. Dang has received the National Institutes of Health/National Cancer Institute MERIT award and numerous other accolades.

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