Synthesis of Misoprostol, and Intramolecular Isomerization of A-Type Misoprostol into B-Type Misoprostol using 1, 8-Diazabicyclo [5.4.0] undec- 7-ene (DBU).

OBJECTIVE: Misoprostol is a synthetic prostaglandin that is related structurally to naturally occurring prostaglandin (PG), and it has been acknowledged as an effective inhibitor of gastric acid secretion when administered intravenously. METHODS: In the present study, the novel application of 1,8-Diazabicyclo[5.4.0]undec-7-ene, a cyclic unsaturated amine [DBU] for the conversion of A-type Misoprostol (A-MP) to B-type Misoprostol (B-MP) via intramolecular isomerization. RESULTS: The intramolecular isomerization process was successfully applied for the separation of enantio-pure isomers with no impurities using DBU. CONCLUSION: The chemical structures of A-MP and B-MP were confirmed using spectral analyses of 1H-NMR, 13C-NMR and Mass spectroscopy.

Harvesting of flow current through implanted hydrophobic PTFE surface within silicone-pipe as liquid nanogenerator.

Harvesting of flow current through implanted hydrophobic surface within silicone pipe as liquid nanogenerators where Tap water (TW), and DI water (DIw) as liquid reservoirs to successfully convert induced mechanical energy into electrical energy. Here, we used a commercial PTFE film for the generation of a hydrophobic surface as a source of mechanical energy. The surface roughness of the hydrophobic surface is confirmed using atomic force microscopy, and contact angle analyses. The generation of power through the interaction of TW and DI with inbuilt PTFE in silicone tube is described. The higher output voltage (Voc), and short circuit currents (Isc) were attained through an interaction of TW and DIw with N-PTFE. The lower Voc, and Isc's were produced when DI water interacts with N-PTFE electrode, whereas TW produced higher Voc and Isc's, respectively, due to a lack of free mobile ions in DIw than TW. The TW-Sh-TENG and DIw-Sh-TENG are produced the maximum peak-to-peak Voc, and Isc of 29.5 V and 17.4 V and 3.7 µA, and 2.9 µA, respectively. Significant power output enhancement of ~ 300% from TW-Sh-TENG from DIw-N-TENG due to the formation of higher surface roughness and lead to the slipping of water droplets by super-hydrophobicity.

Integrated electronic skin (e-skin) for harvesting of TENG energy through push-pull ionic electrets and ion-ion hopping mechanism.

The development of highly durable, stretchable, and steady triboelectric nanogenerators (TENGs) is highly desirable to satisfy the tight requirement of energy demand. Here, we presented a novel integrated polymeric membrane that is designed by PEDOT: PSSa-naphthalene sulfonated polyimide (PPNSP)-EMI.BF4 Electronic skin (e-skin) for potential TENG applications. The proposed TENG e-skin is fabricated by an interconnected architecture with push-pull ionic electrets that can threshold the transfer of charges through an ion-hopping mechanism for the generation of a higher output voltage (Voc) and currents (Jsc) against an electronegative PTFE film. PPNSP was synthesized from the condensation of naphthalene-tetracarboxylic dianhydride, 2,2'-benzidine sulfonic acid, and 4,4'diaminodiphenyl ether through an addition copolymerization protocol, and PEDOT: PSSa was subsequently deposited using the dip-coating method. Porous networked PPNSP e-skin with continuous ion transport nano-channels is synthesized by introducing simple and strong molecular push-pull interactions via intrinsic ions. In addition, EMI.BF4 ionic liquid (IL) is doped inside the PPNSP skin to interexchange ions to enhance the potential window for higher output Voc and Iscs. In this article, we investigated the push-pull dynamic interactions between PPNSP-EMI.BF4 e-skin and PTFE and tolerable output performance. The novel PPNSP- EMI.BF4 e-skin TENG produced upto 49.1 V and 1.03 µA at 1 Hz, 74 V and 1.45 µA at 2 Hz, 122.3 V and 2.21 µA at 3 Hz and 171 V and 3.6 µA at 4 Hz, and 195 V and 4.43 µA at 5 Hz, respectively. The proposed novel TENG device was shown to be highly flexible, highly durable, commercially viable, and a prospective candidate to produce higher electrical charge outputs at various applied frequencies.

Isolation, Characterization, and Docking Studies of (Z)-Isopropyl 7-((1R, 2R, 3R, 5S)- 2-((1E, 3Z)-3-Fluoro-4-Phenoxybuta-1, 3-Dienyl)-3,5-Dihydroxycyclopentyl) Hept-5- Enoate, an Impurity of Tafluprost.

INTRODUCTION: The origin, isolation, and characterization of (Z)-isopropyl 7-((1R, 2R, 3R, 5S)-2-((1E, 3Z)-3-fluoro-4-phenoxybuta-1, 3-dienyl)-3, 5-dihydroxycyclopentyl) hept-5-enoate, an impurity found in the preparation of an anti-glaucoma agent-Tafluprost has been described in this study. MATERIALS AND METHODS: Further, an enantiospecific synthesis of (Z)-isopropyl 7-((1R, 2R, 3R, 5S)-2-((1E, 3Z)- 3-fluoro-4-phenoxybuta-1, 3-dienyl)-3, 5-dihydroxycyclopentyl) hept-5-enoate has been revealed using deoxofluorination as a key transformation of the strategy. RESULTS AND DISCUSSIONS: Moreover, the impurity showing anti-glaucoma properties in docking studies with respect to bimatoprost has been described. CONCLUSION: The extention of our work towards docking studies and the present impurity molecule showed almost the same biological activity with respect to Tafluprost.

Facile Synthetic Protocols for the Preparation of New Impurities in Pemetrexed Disodium Heptahydrate as an Anti-cancer Drug.

A facile synthetic protocol was employed to prepare process-related impurities associated with the synthesis of pemetrexed disodium heptahydrate, Alimta. The research work is described for the development of the novel synthetic methods and their structure elucidation of Pemetrexed glutamide, N-methyl pemetrexed, and N-methyl pemetrexed glutamide impurities. The listed impurities were deduced through spectral analysis, such as 1H-NMR, 13CNMR, and HRMS. The target compounds can be used as the reference substances for quality control.

Reusable Nano-Zirconia-Catalyzed Synthesis of Benzimidazoles and Their Antibacterial and Antifungal Activities.

In this article, a zirconia-based nano-catalyst (Nano-ZrO2), with intermolecular C-N bond formation for the synthesis of various benzimidazole-fused heterocycles in a concise method is reported. The robustness of this reaction is demonstrated by the synthesis of a series of benzimidazole drugs in a one-pot method. All synthesized materials were characterized using 1HNMR, 13CNMR, and LC-MS spectroscopy as well as microanalysis data. Furthermore, the synthesis of nano-ZrO2 was processed using a standard hydrothermal technique in pure form. The crystal structure of nano-ZrO2 and phase purity were studied, and the crystallite size was calculated from XRD analysis using the Debye-Scherrer equation. Furthermore, the antimicrobial activity of the synthesized benzimidazole drugs was evaluated in terms of Gram-positive, Gram-negative, and antifungal activity, and the results were satisfactory.

An aerobic oxidation of alcohols into carbonyl synthons using bipyridyl-cinchona based palladium catalyst.

We have reported an aerobic oxidation of primary and secondary alcohols to respective aldehydes and ketones using a bipyridyl-cinchona alkaloid based palladium catalytic system (PdAc-5) using oxygen at moderate pressure. The PdAc-5 catalyst was analysed using SEM, EDAX, and XPS analysis. The above catalytic system is used in experiments for different oxidation systems which include different solvents, additives, and bases which are cheap, robust, non-toxic, and commercially available on the industrial bench. The obtained products are quite appreciable in both yield and selectivity (70-85%). In addition, numerous important studies, such as comparisons with various commercial catalysts, solvent systems, mixture of solvents, and catalyst mole%, were conducted using PdAc-5. The synthetic strategy of oxidation of alcohol into carbonyl compounds was well established and all the products were analysed using 1H NMR, 13CNMR and GC-mass analyses.

Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihydroisoquinoline-2(1H)-yl)methyl) oxazol-5(4H)-one Derivatives Using 1,2,3,Tetrahydroisoquinoline and their Antimicrobial Activity.

AIMS: A series of six 4-benzylidene-2-((1-phenyl-3,4-dihydro isoquinoline-2(1H)-yl)methyloxazol- 5(4H)-one derivatives were synthesized by condensation of substituted aryl aldehydes with 2-(2-(1-phenyl-3,4- dihydro isoquinoline-2(1H)-acetamido)acetic acid in the presence of sodium acetate, acetic anhydride and zinc oxide as catalysts. BACKGROUND: Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihy droisoquinoline-2(1H)-yl)methyl)oxazol- 5(4H)-one derivatives using 1,2,3,Tetrahydroisoquinoline and their antimicrobial activity. OBJECTIVE: The title compounds can be synthesized from 1,2,3,4-tetrahydroisoquinoline. METHODS: The target molecules, i.e., 4-benzylidene-2-((1-phenyl-3, 4-dihydro isoquinoline-2(1H)-yl) methyl) oxazol-5(4H)-one derivatives (8a-8f) have been synthesized from 1,2,3,4-tetrahydroisoquinoline which was prepared from benzoic acid in few steps. RESULTS: All the six compounds were evaluated based on advanced spectral data (1H NMR, 13C NMR & LCMS), and the chemical structures of all compounds were determined by elemental analysis. CONCLUSION: Antibacterial activity of the derivatives was examined for the synthesized compounds and results indicate that compound with bromine substitution has a good activity profile.

In situ generated hydrophobic micro ripples via π-π stacked pop-up reduced graphene oxide nanoflakes for extended critical heat flux and thermal conductivities.

We report the synthesis of thermally heated pop-up reduced graphene oxide (Pop-rGO) and its nanofluid (Pop-rGO-Nf) in DI water for extended critical heat flux (CHF) in a nucleate pool boiling experiment. When Pop-rGO-Nf is boiled over a nichrome (NiCr) wire heater the CHF values were increased up to 132%, 156%, and 175% with increasing concentrations of 0.0005 vol%, 0.001 vol%, and 0.005 vol% at heat fluxes of q'' = 264 333 kW m-2, 339 202 kW m-2, and 327 895 kW m-2, respectively, because of the higher surface area of 430 m2 g-1. We also found a decrease in the CHF value from 0.05 vol% (175%) to 0.01 vol% (153%) for Pop-rGO-Nf due to the nanofluid concentration reaching the saturation point. After nucleate pool boiling, the developed Pop-rGO-Nf built-up layer on the NiCr wire surface showed regular π-π stacking with novel micro-rippled structures having uniform nanocavities and nanochannels. The nanocavities strongly helped vapor bubbles to escape from the NiCr wire surface. In addition, the nanochannels were formed by hydrogen bonding of adjacent carboxyl groups of each Pop-rGO nanosheet. The surface hydrophobicity of the built-up layers increased with the increase of the concentration of the Pop-rGO-Nfs, and the surface morphology, roughness average (R a) and hydrophobicity were determined using FE-SEM, AFM and contact angle (CA) analysis. In our present investigation, during and after the nucleate CHF experiments with Pop-rGO-Nfs, for the first time, we obtained a higher CHF value of 175% at 0.01 vol% and a higher CA of 118° obtained at 0.05 vol%, due to the increase in surface hydrophobicity and the novel micro-rippled structures. We anticipate that the present results suggest that pool boiling employing Pop-rGO-Nf can dissipate the critical heat flux of electronic chips to a greater extent, allowing the enhancement of the cooling performance in existing two-phase heat transfer devices.

"Fingertip"-guided noncovalent functionalization of carbon nanotubes by dendrons.

Noncovalent functionalization of carbon nanotubes (CNTs) by dendrons was demonstrated. Certain types of dendrons successfully functionalized CNT surfaces through the noncovalent interactions between the peripheries of the dendrons and the sidewalls of CNTs. Dendrons have a unique anisotropic shape and an orthogonal functional group at their apex, and thus can generate a certain spacing between the functional groups upon immobilization on surfaces. Atomic force microscope (AFM) imaging, dispersion experiments, and MicroRaman spectroscopy were employed for the characterization of the functionalization. The binding was found to be governed by the chemical nature of the terminal groups, namely, the "fingertips", through a comparison study on the adsorption efficiency of the dendron analogs. Functional groups such as the carboxylic acid group and the benzyl amide group were effective for the cooperative binding. AFM analysis showed that the average spacing generated by the dendrons was 14-15 nm at a particular adsorption condition. Assembling streptavidin on the tubes through the dendrons and biotin confirmed the realization of the regulated spacing as well as the elimination of unwanted aggregation. The noncovalent functionalization of CNTs by a dendron can be a new approach toward sensible nanobiodevices, not only by introducing biomolecular probes on CNTs without disruption of the electronic network of the tubes, but also by providing the immobilized probe molecules with a space ample enough to minimize steric hindrance for the unhindered interaction with their target species.