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  Subjects -> PHARMACY AND PHARMACOLOGY (Total: 575 journals)
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ISSN (Online) 2509-9396
Published by Thieme Publishing Group Homepage  [233 journals]
  • Boric Acid: A Mild and Efficient Green Catalyst for Organic
    • SynOpen 2023; 07: 290-292
      DOI: 10.1055/a-2110-2785


      Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, Germany

      Artikel in Thieme eJournals:
      Inhaltsverzeichnis     Abstract     open access Volltext

      SynOpen 2023; 07: 290-2922023-07-20T11:38:01+01:00
      Issue No: Vol. 07, No. 03 (2023)
  • Ziegler–Natta Catalysts: Applications in Modern Polymer Science
    • SynOpen 2023; 07: 293-296
      DOI: 10.1055/s-0040-1720078


      Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, Germany

      Artikel in Thieme eJournals:
      Inhaltsverzeichnis     Abstract     open access Volltext

      SynOpen 2023; 07: 293-2962023-07-26T12:55:33+01:00
      Issue No: Vol. 07, No. 03 (2023)
  • Green Synthesis of Pyrazoles: Recent Developments in Aqueous Methods

    • Authors: Singh; Sushma, Yadav, Sidhant, Minakshi, Minakshi, Pundeer, Rashmi
      Pages: 297 - 312
      Abstract: Organic syntheses by adopting green protocols such as sonochemical procedures, microwave technologies, solvent-free conditions, green solvents, heterogeneous catalysis particularly nanocatalysts, ionic liquids have replaced traditional procedures due to concerns pertaining especially to the environment. The heterocycle, pyrazole, due to its multifaceted applications, has been the target of chemists and therefore various synthetic approaches have been developed to synthesize pyrazole-containing molecules. In the present compilation, we have summarized recent water-based research work on the synthesis of pyrazoles.1 Introduction2 Synthesis of Polyfunctionalized Pyrazoles3 Synthesis of Fused Pyrazoles in Water without Catalyst3.1 Fused [5-5]System (3 Heteroatoms): Furo[2,3-c]pyrazoles3.2 Fused [5-6]System (3 Heteroatoms): Pyrano[2,3-c]pyrazoles3.3 Fused [5-6-6]System (3 Heteroatoms): Pyrazolo[3,4-b]quinolones4 Synthesis of Fused Pyrazoles in Water Using Catalyst4.1 Fused [5-5]System (3 Heteroatoms): Furo[2,3-c]pyrazoles4.2 Fused [5-6]System (3 Heteroatoms): Pyrano[2,3-c]pyrazoles4.3 Fused [5-6-6]System (2 Heteroatoms): Pyrazolo[1,2-b]phthalazines4.4 Fused [5-6-6]System (3 Heteroatoms): Benzopyranopyrazoles4.5 Fused [5-6-6]System (5 Heteroatoms): Pyrazolo[4′,3′:5,6]pyrido [2,3- d]pyrimidines and Pyrazolo[4′,3′:5,6]pyrano[2,3-d]pyrimidines5 Conclusions
      Citation: SynOpen 2023; 07: 297-312
      PubDate: 2023-08-07T16:16:25+01:00
      DOI: 10.1055/a-2123-8102
      Issue No: Vol. 07, No. 03 (2023)
  • DMSO arbitrated Oxidative Annulation Followed by Homologated N-Alkylation:
           Microwave-Assisted Efficient and Greener Approach to Access
           3-(3-Oxo-3-arylpropyl) Quinazolinones

    • Authors: Prasanthi; A. V. G., Babu, Bathini Nagendra
      Pages: 313 - 321
      Abstract: A convenient, time efficient, tandem approach for the synthesis of medicinally privileged 3-(3-oxo-3-arylpropyl) quinazolinones is developed from ubiquitously available acetophenones and anthranilamide via microwave irradiation. This transition-metal-free reaction is initiated by the oxidative annulation of anthranilamide and in situ generation of α,β-unsaturated carbonyl compounds from aryl ketones in the presence of K2S2O8 and dimethyl sulfoxide. The latter acts as a source of two carbons [methine (=CH–) and methylene (–CH2–)] apart from being the solvent. The reaction is carried out under microwave irradiation which has the advantage of homogenous heat distribution, reducing the reaction time drastically compared to the conventional heating reaction.
      Citation: SynOpen 2023; 07: 313-321
      PubDate: 2023-08-08T15:24:14+01:00
      DOI: 10.1055/s-0040-1720079
      Issue No: Vol. 07, No. 03 (2023)
  • Recent Advances in the Synthesis of Bioactive Glycohybrids via

    • Authors: Singh; Kavita, Tyagi, Rajdeep, Mishra, Vinay Kumar, Tiwari, Ghanshyam, Sagar, Ram
      Pages: 322 - 352
      Abstract: Carbohydrates, traditionally known for their energy-providing role, have gained significant attention in drug discovery due to their diverse bioactivities and stereodiversity. However, pure carbohydrate molecules often exhibit limited bioactivity and suboptimal chemical and physical characteristics. To address these challenges, functional groups with bioactive scaffolds have been incorporated into carbohydrate to enhance their bioactivity and improve their overall properties. Among the various synthetic methods available, click chemistry has emerged as a powerful tool for the synthesis of carbohydrate-containing bioactive scaffolds, known as glycohybrids. Click chemistry offers several advantages, including high chemo- and regioselectivity, mild reaction conditions, easy purification, and compatibility with multiple functional groups. In the present review, we have emphasized the recent advances and most pertinent research on the development of 1,2,3-triazole-containing glycohybrids using the click reaction, their biological evaluations and the structure-activity relationship during 2017–2023. These newly synthesised glycohybrids could potentially be developed as new chemical entities (NCE) in pharmaceutical chemistry and may encourage the use of carbohydrates in drug discovery processes.1 Introduction2 CuAAC Click Chemistry Mediated Synthesis of Triazole-Based Glycohybrids and their Biological Activities3 Conclusions and Perspective
      Citation: SynOpen 2023; 07: 322-352
      PubDate: 2023-08-10T10:57:59+01:00
      DOI: 10.1055/a-2130-7319
      Issue No: Vol. 07, No. 03 (2023)
  • Heterogeneous Catalysis for Sustainable Energy

    • Authors: Tuteja; Jaya
      Pages: 353 - 361
      Abstract: The dominance of fossil fuels in the energy sector is associated with greenhouse-gas emission and release of atmospheric pollutants. Biomass-based energy generation is considered a potential alternative for replacement of fossil fuels, and it has been used as a sustainable source of heat and power for a long time. Biomass as a feedstock can be used for the synthesis of different energy products. Catalysts play a significant role in various conversion routes and affect the yield of major products. Researchers have mainly focused on starchy feedstock, lignocellulosic biomass, and triglyceride containing biomass for bioenergy production. Catalytic reactions for biomass feedstock mainly involve deoxygenation, hydrolysis, hydrogenation, dehydrogenation, and oxidation etc. This review provides an overview of catalytic reactions for the conversion of different classes of biomass feedstock for biofuel production. The primary aim of this review is to summarize catalytic strategies for conversion of lignocellulosic biomass into value-added products.
      Citation: SynOpen 2023; 07: 353-361
      PubDate: 2023-08-10T11:06:56+01:00
      DOI: 10.1055/a-2129-9076
      Issue No: Vol. 07, No. 03 (2023)
  • Multi-step Flow Synthesis of the Anthelmintic Drug Praziquantel

    • Authors: Phull; Manjinder Singh, Jadav, Surender Singh, Bohara, Chander Singh, Gundla, Rambabu, Mainkar, Prathama S
      Pages: 362 - 370
      Abstract: Praziquantel (PZQ; Brand name: Biltricide) is categorized as an anthelminthic drug, and it is used for the treatment of Schistosomiasis and other parasitic infections. The World Health Organization (WHO) has classified it as one of the essential and emergency medicines needed across the globe. The price of PZQ formulated product depends on the associated method of preparation, along with cost of raw materials. A precise and reliable method for the preparation of PZQ using a flow-chemistry approach is described in this study using phenylethylamine as the starting material. The main objective of the present study is to identify a new economical route for the synthesis of PZQ that could decrease the production time drastically from days to minutes and be transferred to large-scale production. Simultaneously, the purity of the obtained intermediates in essential steps, as single or continuous process, determined by HPLC analysis were more than 90% pure. The continuous preparation process of PZQ in the current study was achieved in less time (ca. 3–4 h) than using conventional methods (ca. 3–4 days). Moreover, the required quantity of key intermediate dimethoxyethanamine is 40–50% less than in existing methods.
      Citation: SynOpen 2023; 07: 362-370
      PubDate: 2023-08-14T14:28:05+01:00
      DOI: 10.1055/s-0042-1751479
      Issue No: Vol. 07, No. 03 (2023)
  • Copper Sulfate (CuSO4): An Efficient Reagent in Organic Synthesis
    • SynOpen 2023; 07: 371-373
      DOI: 10.1055/a-2134-9007


      Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, Germany

      Artikel in Thieme eJournals:
      Inhaltsverzeichnis     Abstract     open access Volltext

      SynOpen 2023; 07: 371-3732023-08-15T13:35:56+01:00
      Issue No: Vol. 07, No. 03 (2023)
  • Sustainable Organocatalyzed Enantioselective Catalytic Michael Additions
           in Betaine-Derived Deep Eutectic Solvents

    • Authors: Fonseca; Daniela P., Amorim, Ana C., Carreiro, Elisabete P., Ramalho, João P. Prates, Hermann, Gesine J., Federsel, Hans-Jürgen, Duarte, Ana Rita C., Burke, Anthony J.
      Pages: 374 - 380
      Abstract: The organocatalyst cinchonidine-squaramide was immobilized within three different deep eutectic solvents (DESs): betaine:d-sorbitol:water, betaine: d-xylitol:water, and betaine:d-mannitol:water and evaluated in a well-known asymmetric Michael addition. These reactions provided excellent yields (up to 99%) and enantioselectivities (up to 98%) using only 1 mol% of organocatalyst. It was also possible to achieve 9 cycles in reactions with DES (betaine:d-sorbitol:water), proving the high recyclability of this system. In the reactions realized with only 0.5 mol% of organocatalyst, it was possible to achieve 5 cycles, and the products were obtained with high yields (up to 95%) and excellent enantioselectivities (up to 94%), using DES (betaine:d-sorbitol:water).
      Citation: SynOpen 2023; 07: 374-380
      PubDate: 2023-08-17T13:39:50+01:00
      DOI: 10.1055/a-2117-9971
      Issue No: Vol. 07, No. 03 (2023)
  • Synthesis of the Key Saccharide Fragments of the Glucuronic
           Acid-Containing Repeat Unit of Pentosan Polysulfate, a Heparin Sulfate

    • Authors: Banwell; Martin G., Marshall, Sarah, Ward, Jas S., Schwartz, Brett D.
      Pages: 381 - 393
      Abstract: Suitably protected mono- and di-saccharide residues associated with the glucuronic acid-containing repeat unit related to pentosan polysulfate have been prepared. The stereo-controlled coupling, using trichloroacetimidate chemistry, of certain of these is also described and the structure of a disaccharide so-formed has been confirmed by single-crystal X-ray analysis.
      Citation: SynOpen 2023; 07: 381-393
      PubDate: 2023-08-21T10:55:43+01:00
      DOI: 10.1055/a-2126-0346
      Issue No: Vol. 07, No. 03 (2023)
  • Synthesis of Novel Phosphorus-Substituted Stable Isoindoles by a
           Three-Component Coupling Reaction of ortho-Phthalaldehyde,
           9,10-Dihydro-9-oxa-10-phosphaphenanthrene 10-Oxide, and Primary Amines

    • Authors: Nakao; Michiyasu, Nakamura, Akihito, Takesue, Tomoyuki, Kitaike, Syuji, Ito, Hiro-O, Sano, Shigeki
      Pages: 394 - 400
      Abstract: A three-component coupling reaction of ortho-phthalaldehyde, 9,10-dihydro-9-oxa-10-phosphaphenanthrene 10-oxide, and various primary amines readily afforded novel phosphorus-substituted stable isoindoles in good to excellent yields. The importance of the reversible ring-opening of 9,10-dihydro-9-oxa-10-phosphaphenanthrene 10-oxide by methanolysis in the three-component coupling reaction became apparent.
      Citation: SynOpen 2023; 07: 394-400
      PubDate: 2023-08-28T11:59:46+01:00
      DOI: 10.1055/a-2148-9433
      Issue No: Vol. 07, No. 03 (2023)
  • Synthesis of Squaric Acid Monoamides as Building Blocks for Drug Discovery

    • Authors: Long; Nathan, Le Gresley, Adam, Solomonsz, Arran, Wozniak, Antony, Brough, Steve, Wren, Stephen P.
      Pages: 401 - 407
      Abstract: Herein, we present a synthetic compound library comprising of 28 anilino and benzylamino monosquarate-amide derivatives. Members of this library were designed as bioisosteric replacements for groups such as the ubiquitous carboxylic acid moiety. Further to their synthesis, we have shown the potential of these chemical building blocks for the generation of additional novel compounds. This work forms part of our efforts aimed at the assembly of 96-well plates loaded with bioisosteric analogues that may be used to enrich drug discovery programs. The research presented in this work focuses on the chemistry of 3,4-dihydroxycyclobut-3-ene-1,2-dione, a known carboxylic acid bioisostere.
      Citation: SynOpen 2023; 07: 401-407
      PubDate: 2023-08-29T15:03:11+01:00
      DOI: 10.1055/a-2148-9518
      Issue No: Vol. 07, No. 03 (2023)
  • Recent Applications of TEMPO in Organic Synthesis and Catalysis

    • Authors: Varala; Ravi, Seema, Vittal
      Pages: 408 - 413
      Abstract: In this spotlight article, authors highlighted the applications of TEMPO in organic synthesis and catalysis starting from 2015 to date.
      Citation: SynOpen 2023; 07: 408-413
      PubDate: 2023-09-07T09:46:08+01:00
      DOI: 10.1055/a-2155-2950
      Issue No: Vol. 07, No. 03 (2023)
  • Pyrrolidinium Acetate (PyrrIL) as a Green and Recyclable Catalyst:
           Synthesis of 2-Phenyl Benzimidazoles and 2-Phenyl Benzothiazoles under
           Solvent-Free Conditions at Room Temperature

    • Authors: Katla; Ramesh, Katla, Rakhi
      Pages: 414 - 421
      Abstract: Benzimidazoles and benzothiazoles are a class of pharmacologically potential compounds, which exhibited antimicrobial, anticancer, and anti-inflammatory activities. These can be obtained by simple condensation of o-phenylenediamine or o-aminothiophenol with aromatic aldehydes. The synthetic protocol can be accomplished/improved by varying reaction parameters such as temperature, solvents, and catalysts. To develop such condensation reactions in a sustainable way, nontoxic solvents and eco- friendly catalysts are presently used. In this study, we proposed a novel and interesting strategy for obtaining diversely substituted 2-phenyl benzimidazole and 2-phenyl benzothiazole derivatives via a one-pot protocol, employing pyrrolidinium ionic liquid as a green and environmentally benign catalyst under solvent-free conditions at room temperature in an open atmosphere. The resulting products were obtained in good to excellent yields within a short reaction time (3–20 min). A plausible mechanism was also discussed.
      Citation: SynOpen 2023; 07: 414-421
      PubDate: 2023-09-08T09:54:17+01:00
      DOI: 10.1055/a-2149-4113
      Issue No: Vol. 07, No. 03 (2023)
  • Synthesis of Calix[4]arene Appended Lactosylated G1 and Galacto­sylated
           G2 Generation Glycodendrimers using a ‘CuAAC’ Click Approach

    • Authors: Kumar; Sunil, Yadav, Mangal S., Singh, Sumit K., Rajkhowa, Sanchayita, Tiwari, Vinod K.
      Pages: 145 - 153
      Abstract: A modular and highly reliable click approach is applied for the expeditious synthesis of lactose- and galactose-coated calixarene-cored G1 and G2 generation glycodendrimers, respectively. The developed calixarene glycodendrimers have been characterized by using extensive spectral analysis including NMR (1H and 13C), MS, IR, and SEC data.
      Citation: SynOpen 2023; 07: 145-153
      PubDate: 2023-04-24T15:28:33+01:00
      DOI: 10.1055/a-2063-4139
      Issue No: Vol. 07, No. 02 (2023)
  • Recent Advancements in Triazole-based Click Chemistry in Cancer Drug
           Discovery and Development

    • Authors: Kumar; Arun, Yadav, Ashok Kumar, Mishra, Vivek, Kumar, Deepak
      Pages: 186 - 208
      Abstract: Triazole-based compounds possess a broad range of activity and can be synthesized using click chemistry. Many new chemotherapeutic agents have been developed in recent years by exploiting click chemistry and these are covered in this review.
      Citation: SynOpen 2023; 07: 186-208
      PubDate: 2023-05-17T15:24:42+01:00
      DOI: 10.1055/s-0042-1751452
      Issue No: Vol. 07, No. 02 (2023)
  • Synthesis of Bioactive Macrocycles Involving Ring-Closing Metathesis

    • Authors: Jahan; Nasrin, Ansary, Inul
      Pages: 209 - 242
      Abstract: This review reports the synthesis of various bioactive macrocycles, involving ring-closing metathesis as a key step, developed since ca. 2000. These macrocycles exhibited biological activities such as antiviral, antifungal, antibacterial, and anticancer activities, and more. Thus, their syntheses and utilization are essential for both synthetic organic and medicinal chemists.
      Citation: SynOpen 2023; 07: 209-242
      PubDate: 2023-05-23T11:41:09+01:00
      DOI: 10.1055/s-0042-1751453
      Issue No: Vol. 07, No. 02 (2023)
  • Click-Chemistry-Assisted Alteration of Glycosaminoglycans for Biological

    • Authors: Bera; Smritilekha, Mondal, Dhananjoy
      Pages: 277 - 289
      Abstract: This short review describes the assistance of click chemistry in the chemical modification of glycosaminoglycans. Through an alkyne-azide 1,3-dipolar cycloaddition reaction, the chemically and physiologically stable triazole unit connects glycosaminoglycans with other labelled or attached functionalities. The synthesized glycosaminoglycan (GAG) conjugates act as drug carriers, forming hydrogels or nanohydrogels for localized drug delivery or injectable GAGs and so on. These are used in research on antithrombotic agents, protein binding, and hepatocyte growth factors, as well as in mechanistic studies of glycosaminoglycans biosynthesis and wound healing.1 Introduction2 Synthetic Modification of GAGS3 Click Chemistry4 Modification of GAGS Applying Click Chemistry5 Conclusions6 Abbreviations
      Citation: SynOpen 2023; 07: 277-289
      PubDate: 2023-06-19T11:30:17+01:00
      DOI: 10.1055/s-0040-1720072
      Issue No: Vol. 07, No. 02 (2023)
  • A Chitosan Hydrochloride Mediated, Simple and Efficient Approach for the
           Synthesis of Hydrazones, their in vitro Antimycobacterial Evaluations, and
           Molecular Modeling Studies (Part III)

    • Authors: Mali; Suraj N., Pandey, Anima, Thorat, Bapu
      Abstract: A simple, eco-friendly and straightforward synthesis of hydrazones has been devised that is conducted in the presence of chitosan Hydrochloride (chitosan·HCl) as catalyst in aqueous-ethanol medium at room temperature. The current protocol offers metal-free synthesis, adaptability to large-scaleup, good yields, and quicker reaction time. All ten synthesized hydrazones also showed good antimycobacterial activity, with minimum inhibitory concentrations (MICs) ranging from 3.12 to 6.25 μg/mL. One of the products presented strong binding affinity against M. tuberculosis pantothenate synthetase (pdb id: 3IVX) with a Glide docking score of –8.803 kcal/mol. Molecular dynamics simulation analysis of its complex with 3IVX retained good stability over the simulation period of 20 ns.
      Citation: SynOpen 2023; :
      PubDate: 2023-03-07T10:49:29+0100
      DOI: 10.1055/a-2035-6493
  • Photochemical Synthesis of Pyrazolines from Tetrazoles in Flow

    • Authors: Burke; Adam, Spiccio, Silvia, Di Filippo, Mara, Baumann, Marcus
      Abstract: Pyrazolines and their pyrazole congeners are important heterocyclic building blocks with numerous applications in the fine chemical industries. However, traditional routes towards these entities are based on multistep syntheses generating substantial amounts of chemical waste. Here we report an alternative approach using UV-light to convert tetrazoles into pyrazolines via a reagent-free photo-click strategy. This route generates nitrile imine dipoles in situ that are trapped with different dipolarophiles rendering a selection of these heterocyclic targets in high chemical yields. A continuous flow method is ultimately realized that generates multigram quantities of product in a safe and readily scalable manner thus demonstrating the value of this photochemical approach for future exploitations in industry.
      Citation: SynOpen 2023; :
      PubDate: 2023-02-22T08:33:15+0100
      DOI: 10.1055/a-1995-1859
  • Click-Type Synthesis of Homoconjugated Push–Pull Chromophores:
           Computational Investigation of Optical and Nonlinear Optical (NLO)

    • Authors: Inyurt; Fevzi Can, Mammadova, Flora, Dengiz, Cagatay
      Abstract: Homoconjugated push–pull chromophores were obtained by an efficient, click-type formal [2+2] cycloaddition. With these short synthetic transformations, complex chromophore structures were achieved in a single step without any by-product formation. Significant second-order optical nonlinearities have been calculated for the synthesized compounds.
      Citation: SynOpen 2023; :
      PubDate: 2023-01-24T11:41:46+0100
      DOI: 10.1055/a-2004-6344
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