scholarly journals MICROWAVE ASSISTED SYNTHESIS, A GREEN PROTOCOL FOR DEVELOPMENT OF NEW AND ADVANCED DRUG DELIVERY SYSTEMS, A REVIEW

2015 ◽  
Vol 3 (9SE) ◽  
pp. 1-4
Author(s):  
KalpanaVirendra Singh
Keyword(s):  
Reaction Times ◽  
Chemical Processes ◽  
Environmentally Benign ◽  
Reaction Pathways ◽  
Microwave Assisted Synthesis ◽  
Primary Concern ◽  
Green Protocol ◽  
Microwave Assisted ◽  
Chemistry Community ◽  
Complex Drug

Medicinal Chemistry community is considering new chemical processes, which are environmentally benign. Environmentally benign synthetic protocols have become the primary concern during complex drug discovery processes. Green chemistry is providing algorithms for protecting the environment, not by cleaning it, but by inventing new chemical processes that fuel the Economy and lifestyles, without causing any damage to the environment. Microwave assisted techniques has opened up new opportunities to the synthetic chemists in the form of new improved reaction pathways, that are not otherwise feasible. MAOS has reduced the reaction times from hours or days to minutes leading to efficient economic way for synthesis of large number of molecules. Present Review article attempts to focus on what is MAOS, how it is generated and works going on in this area.

Microwave-assisted synthesis of zinc 5-(4-carboxyphenyl)-10,15,20-triphenylporphyrin and zinc 5-(4-carboxyphenyl)-10,15,20-triphenylchlorin

2015 ◽  
Vol 19 (04) ◽  
pp. 595-600 ◽  
Author(s):  
Rima Chouikrat ◽  
Aymeric Champion ◽  
Régis Vanderesse ◽  
Céline Frochot ◽  
Albert Moussaron
Keyword(s):  
Reaction Times ◽  
Microwave Assisted Synthesis ◽  
Spectroscopic Techniques ◽  
H Nmr ◽  
Microwave Assisted ◽  
Experimental Protocols ◽  
Time Of Reaction

The microwave-assisted synthesis of zinc 5-(4-carboxyphenyl)-10,15,20-triphenylporphyrin and zinc 5-(4-carboxyphenyl)-10,15,20-triphenylchlrorin are described and compared to classic conditions of synthesis in terms of time of reaction and yields obtained. The new experimental protocols are easy to implement required small amounts of reagents and solvents and lead to short reaction times. All compounds have been characterized by 1 H NMR, MS and spectroscopic techniques.

scholarly journals Green Chemistry Approach for Efficient Synthesis of Schiff Bases of Isatin Derivatives and Evaluation of Their Antibacterial Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Jnyanaranjan Panda ◽  
V. Jagannath Patro ◽  
Biswa Mohan Sahoo ◽  
Jitendriya Mishra
Keyword(s):  
Green Chemistry ◽  
Schiff Bases ◽  
Reaction Times ◽  
Antibacterial Activities ◽  
Primary Amines ◽  
Microwave Assisted Synthesis ◽  
Azomethine Group ◽  
Microwave Assisted ◽  
Isatin Derivatives

Microwave-assisted organic synthesis, a green chemistry approach, is nowadays widely used in the drug synthesis. Microwave-assisted synthesis improves both throughput and turnaround time for medicinal chemists by offering the benefits of drastically reduced reaction times, increased yields, and pure products. Schiff bases are the important class of organic compounds due to their flexibility, and structural diversities due to the presence of azomethine group which is helpful for elucidating the mechanism of transformation and rasemination reaction in biological system. This novel compound could also act as valuable ligands for the development of new chemical entities. In the present work, some Schiff bases of Isatin derivatives was synthesized using microwave heating method. Schiff base of Isatin were synthesized by condensation of the keto group of Isatin with different aromatic primary amines. They were characterized by means of spectral data and subsequently subjected to the in vitro antibacterial activities against gram positive and gram negative strains of microbes. It was observed that the compound with electron withdrawing substituents exhibited good antibacterial activities against almost all the micro organisms.

scholarly journals Microwave Assisted Synthesis of Six Member Ring Azaheterocycles and Their Antimycobacterial and Anticancer Evaluation

2001 ◽  
Vol 71 (3) ◽  
pp. 287-293 ◽  
Author(s):  
Cristina Al Matarneh ◽  
Catalina-Ionica Ciobanu ◽  
Violeta Mangalagiu ◽  
Gheorghita Zbancioc ◽  
Ramona Danac
Keyword(s):  
Breast Cancer ◽  
Prostate Cancer ◽  
Lung Cancer ◽  
Renal Cancer ◽  
Reaction Times ◽  
Antimycobacterial Activity ◽  
Microwave Assisted Synthesis ◽  
Thermal Heating ◽  
Microwave Assisted ◽  
Mw Irradiation

We report herein a comparative study concerning the influence of microwave (MW) irradiation comparative with conventional thermal heating (TH) in the reaction of six member ring azaheterocycles (derived from phenanthroline, quinoline, isoquinoline and phthalazine) with ethyl cyanoformate, and their anticancer and antimycobacterial activity. Under MW irradiation the reactions have some undeniable advantages: the reaction times decrease dramatically (from hours to minutes), the yields are higher, the reactions became selective in some cases (4,7-phenanthrolinium and phthalazinium ylides). The decreasing of reaction time+ from hours to minutes corroborated with the fact that in majority of cases the yield are higher and the selectivity is better, allow us to say that these reactions could be considered as eco-friendly. As far for biological activity, three of the compounds exhibited a significant antitumor activity against some cancer cell lines including prostate cancer, leukemia, renal cancer, lung cancer and breast cancer. The best potency in terms of growth inhibition of tumor cells (~45%) was shown by compound 4a against renal cancer A498 and ovarian cancer SK-OV-3 cells. The tested compounds have not shown any antimycobacterial activity against Mycobacterium tuberculosis.

scholarly journals Microwave Assisted Synthesis of Quinoline Fused Benzodiazepines as Anxiolytic and Antimicrobial Agents

2021 ◽  
Vol 33 (5) ◽  
pp. 1107-1114
Author(s):  
S.B. Marganakop ◽  
R.R. Kamble ◽  
A.R. Nesaragi ◽  
P.K. Bayannavar ◽  
S.D. Joshi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Docking Studies ◽  
K Channel ◽  
Microwave Assisted Synthesis ◽  
Green Protocol ◽  
Microwave Assisted ◽  
Consensus Score ◽  
Surflex Docking

In the present study, an efficient, facile and green protocol for synthesis of quinoline fused 1,4-benzodiazepine (4a-j) by microwave irradiated condensation of 6/7/8-substituted 3-bromomethyl- 2-chloro-quinoline (3a-j) obtained from 2-chloro 6/7/8-substituted quinoline-3-carbaldehyde (1a-j) with 1, 2-phenylenediamine was developed. Surflex docking studies with K+ channel is one of the physiological targets and inhibition, which plays a role in the pathophysiology of depression revealed that all these compounds show consensus score in the range 2.71-3.68 indicating the summary of all forces of interaction. Further, compounds 4d, 4g and 4i exhibited potent antibacterial activity

scholarly journals Green, Microwave-Assisted Synthesis of O-Perbutyrylated-Alkyl-Glycosides

Proceedings ◽  
2019 ◽  
Vol 41 (1) ◽  
pp. 42
Author(s):  
Emmanuel Pérez-Escalante ◽  
Luis Guillermo González-Olivares ◽  
Araceli Castañeda-Ovando ◽  
Verónica Salazar-Pereda ◽  
John F. Trant ◽  
...  
Keyword(s):  
Lewis Acids ◽  
Model Compound ◽  
Traditional Approach ◽  
Reaction Times ◽  
Conventional Heating ◽  
Microwave Assisted Synthesis ◽  
Hydroxyl Groups ◽  
Alkyl Glycosides ◽  
Microwave Assisted ◽  
Synthetic Strategy

Chemical synthesis of carbohydrates is a challenging task. Several protection and deprotection steps of hydroxyl groups are required to ensure regioselective formation of the glycosidic bond. Usually, it is achieved through acylation, where conventional heating is combined with addition of Lewis acids as catalysts. This traditional approach has two drawbacks; it is time consuming and often catalysts are hazardous to the environment. An alternative route relies on application of microwaves and/or other Lewis acids with less or no toxicity. Such combination would reduce reaction times and offer a benign synthetic strategy to obtain peracylated compounds. The current work describes an efficient and environmentally mild synthesis of peracylated glycosides with potential application in enzymatic preparation of carbohydrates. Model compound O-perbutyrylated-phenyl-galactose was synthesized using imidazole as catalyst in the microwave-assisted process. The acylation protocol was optimized, and the target sugar was obtained at 50% yield after 1 h. In conclusion, the combination of imidazole and microwaves provides an excellent alternative to swiftly synthesize peracylated glycosides in a benign way.

Microwave-Assisted Synthesis of Azo Aromatic Diacyl Chlorides

2012 ◽  
Vol 524-527 ◽  
pp. 1702-1705
Author(s):  
Qing Chao Jia ◽  
Yan Jun Chen ◽  
Hong Min Hou
Keyword(s):  
Microwave Irradiation ◽  
Ultrasonic Irradiation ◽  
Reaction Times ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted

Six azo aromatic diacyl chlorides were synthesized under microwave irradiation. The method offers better yields in shorter reaction times compared to classical heating approaches and ultrasonic irradiation.

scholarly journals Technetium and rhenium schiff base complexes for nuclear medicine

2019 ◽  
Author(s):  
◽  
Jakob Edwin Baumeister
Keyword(s):  
Nuclear Medicine ◽  
Schiff Base ◽  
Reaction Times ◽  
Mixed Ligand ◽  
Schiff Base Complexes ◽  
Microwave Assisted Synthesis ◽  
One Pot ◽  
Diverse Range ◽  
Microwave Assisted ◽  
Potential Applications

This dissertation investigates the synthesis of rhenium and technetium Schiff base complexes for potential applications in nuclear medicine. In Chapter 2, a series of mixed ligand Re(III) complexes of the form trans-[Re(PR3)2(tmf2en)]+ were prepared by microwave assisted synthesis. A two-step (one-pot) procedure was utilized. In the first step, the Re(V) precursor (nBu4N)[ReOCl4] is reacted with the Schiff base ligand forming trans-[ReOCl(tmf2en) in situ. In the second step, a tertiary phosphine ligand is added yielding the reduced trans-[Re(PR3)2(tmf2en)][superscript +] species. The preparation of these trans-[Re(PR3)2(tmf2en)][superscript +] complexes by microwave assisted synthesis resulted in higher reaction yields and shorter reaction times compared to syntheses of similar Re(III) Schiff base complexes. The general methodology proved to be useful for the synthesis of mixed ligand Re(III) complexes with a diverse range of Schiff base ligands and phosphines.

scholarly journals Microwave-assisted synthesis of 2-substituted 4,5,6,7-tetrahydro-1,3-thiazepines from 4-aminobutanol

2020 ◽  
Vol 16 ◽  
pp. 32-38
Author(s):  
María C Mollo ◽  
Natalia B Kilimciler ◽  
Juan A Bisceglia ◽  
Liliana R Orelli
Keyword(s):  
General Procedure ◽  
Reaction Times ◽  
Solvent Free ◽  
Ring Closure ◽  
Microwave Assisted Synthesis ◽  
Microwave Assisted ◽  
Solvent Free Conditions

A general procedure for the synthesis of 2-substituted tetrahydro-1,3-thiazepines by MW-assisted cyclization of 4-thioamidobutanols is presented. The acyclic precursors were prepared in high overall yields by an expeditious three-step diacylation/thionation/deprotection sequence from 4-aminobutanol. Microwave-assisted ring closure of 4-thioamido alcohols promoted by trimethylsilyl polyphosphate (PPSE) in solvent-free conditions allowed for the synthesis of several hitherto unreported seven-membered iminothioethers bearing 2-aryl, alkenyl, aralkyl and alkyl substituents. The cyclodehydration reaction is likely to involve an SN2-type displacement and affords good to excellent yields of the desired heterocycles in very short reaction times.

scholarly journals MICROWAVE-ASSISTED SYNTHESIS, CHARACTERIZATION, AND BIOLOGICAL EVALUATION OF PHENYLACRYLAMIDE DERIVATIVES OF TRIAZOLES DERIVED FROM OXAZOLONES

2018 ◽  
Vol 11 (7) ◽  
pp. 285
Author(s):  
Venkat Swamy Puli ◽  
Vukoti Kiran Kumar ◽  
Venkata Reddy Regalla ◽  
Anindita Chatterjee
Keyword(s):  
Antioxidant Activities ◽  
Reaction Times ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Spectral Studies ◽  
Microwave Assisted Synthesis ◽  
Microwave Technology ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
Derivatives Of

Objective: The aim of the present study is to synthesize novel phenylacrylamide derivatives as potent bioactive agents.Methods: Novel N-(3-(4H-1,2,4-triazol-4-ylamino)-3-oxo-1-arylidene prop-2-yl) benzimidic acids (7a-c) have been synthesized by the reaction of 4-(arylidene)-2-phenyloxazol-5(4H)-ones (5a-c) with 4-amino-1, 2, 4-triazole (6) in the presence of anhydrous sodium acetate in glacial acetic acid. Titled compounds (7a-c) were obtained in good yields using microwave technology which resulted in dramatic reductions in reaction times leading to the formation of phenylacrylamide derivatives (7a-c) at a faster rate.Results: The structures of the newly synthesized compounds were characterized by Fourier-transform infrared, 1H NMR, 13C NMR, and mass spectral studies. This method can be an efficient method for the synthesis of phenylacrylamide derivatives (7a-c).Conclusion: All the final compounds were screened for their antimicrobial and antioxidant activities and found to be biologically active. Among all the compounds, 7b was found to be potent antimicrobial and antioxidant.

Microwave-assisted Synthesis of N-phenylanthranilic Acids in Water

2005 ◽  
Vol 2005 (9) ◽  
pp. 561-563 ◽  
Author(s):  
Ana Martín ◽  
Rolando F. Pellón ◽  
Miriam Mesa ◽  
Maite L. Docampo ◽  
Victoria Gómez
Keyword(s):  
Microwave Irradiation ◽  
Aqueous Media ◽  
Reaction Times ◽  
Microwave Assisted Synthesis ◽  
Chlorobenzoic Acid ◽  
Microwave Assisted ◽  
Aniline Derivatives ◽  
Water As Solvent

N-Phenylanthranilic acid derivatives were synthesised using the Ullmann condensation of 2-chlorobenzoic acid with aniline derivatives under microwave irradiation in aqueous media. The method offers better yields in shorter reaction times compared to classical heating approaches using water as solvent.

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