Stereoselective Synthesis of Highly Functionalized Aminobenzothiazole-Fused Spirooxindole Derivatives: in silico and in vitro Anti-Diabetic Studies
Synthesis DOI: 10.1055/a-2161-0283 A series of highly functionalized spirooxindole pyrrolizidine/pyrrolothiazole derivatives have been synthesized by the three-component 1,3-dipolar cycloaddition reaction of benzothiazolyl amides with isatin-based azomethine ylides. The pharmacologically significant spirooxindole derivatives bearing one quaternary carbon and four stereocenters were obtained in excellent yields (up to 93%). The compounds were screened for their anti-diabetic activity against two enzymes, α-glucosidase and α-amylase. The results exhibited potent inhibitory activity against these enzymes, especially N-(be...
Source: Synthesis - October 4, 2023 Category: Chemistry Authors: Nivetha, Narayanasamy Patil, Shashank M. Ramu, Ramith Sreenivasa, Swamy Velmathi, Sivan Tags: paper Source Type: research
Visible-Light-Mediated Oxidation of 1-Benzyl-3,4-dihydroisoquinolines with Dioxygen: A Switchable Synthesis of 1-Benzoylisoquinolines and 1-Benzoyl-3,4-dihydroisoquinolines
Synthesis DOI: 10.1055/a-2160-8903 A visible-light-mediated metal-free oxidation of 1-benzyl-3,4-dihydroisoquinolines (1-BnDHIQs) for the switchable preparation of a wide range of 1-benzoylisoquinolines (BzIQs) and 1-benzoyl-3,4-dihydroisoquinolines (BzDHIQs) is realized using dioxygen as the oxidant. This protocol provides a facile route for the efficient synthesis of isoquinoline alkaloids. Mechanistic investigations suggest that a radical pathway and an ionic pathway may exist simultaneously, with both pathways proceeding via a common key peroxide intermediate to give the oxidized products. [...] Georg Thieme Verlag KG ...
Source: Synthesis - October 4, 2023 Category: Chemistry Authors: Ma, Peipei Wu, Hongli Gan, Haifeng Tags: paper Source Type: research
Recent Advancements in Typical Friedel –Crafts Alkylation Reactions Focused on Targeting Arene Nucleophiles
Conclusion and Outlook [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Synthesis)
Source: Synthesis - October 2, 2023 Category: Chemistry Authors: Singh, Sanjay Hazra, Chinmoy K. Tags: short review Source Type: research
Efficient Synthesis of Chirally Enriched 1H-Imidazo[1,2-b]pyrazole- and 4H-Imidazo[1,2-b][1,2,4]triazole-Based Bioactive Glycohybrids
Synthesis DOI: 10.1055/a-2157-9100 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, bioactive scaffolds have been incorporated into carbohydrate to enhance their bioactivity and improve their overall properties. Among the various heterocyclic structural motifs known for their pharmacological properties, imidazo-pyrazole and imidazo-triazole skelet...
Source: Synthesis - October 2, 2023 Category: Chemistry Authors: Mishra, Vinay Kumar Tiwari, Ghanshyam Khanna, Ashish Tyagi, Rajdeep Sagar, Ram Tags: paper Source Type: research
Recent Advances on High-Order Dipolar Annulations of Donor –Acceptor Cyclopropanes/Cyclobutanes
Conclusion [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Synthesis)
Source: Synthesis - September 28, 2023 Category: Chemistry Authors: Yang, Liangliang Wang, Haiyang Lang, Ming Peng, Shiyong Tags: short review Source Type: research
Palladium/Charcoal-Catalysed Olefin Reduction for the Simple and Efficient Synthesis of Substituted gem-Diborylalkanes
Synthesis DOI: 10.1055/a-2147-1336
gem-Diborylalkanes have recently emerged as valuable synthons for diverse C–C bond-forming reactions. They represent an important class of bifunctional reagents that can be applied for the synthesis of simple to complex skeletons. Herein, we report a Pd-catalysed hydrogenation method for the synthesis of gem-diborylalkanes from the corresponding gem-diborylalkenes, which are themselves prepared from the corresponding aldehydes and ketones using known procedures. In addition, transformations of two representative gem-diborylalkane products are discussed leading to a range of funct...
Source: Synthesis - September 28, 2023 Category: Chemistry Authors: Das, Kanak Kanti Ghorai, Debraj Mahato, Somenath Panda, Santanu Tags: paper Source Type: research
Recent Developments on the Synthesis of Sulfoxides via Sulfenate Anions
Conclusions and Outlook [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Synthesis)
Source: Synthesis - September 27, 2023 Category: Chemistry Authors: Saito, Fumito Tags: short review Source Type: research
Synthesis of Pyrido[2,3-d]pyrimidines Catalyzed by 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone (DDQ)/tert-Butyl Nitrite (TBN)/O2
Synthesis DOI: 10.1055/a-2156-7470 Catalyzed by 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ)/tert-butyl nitrite (TBN)/O2, an efficient tandem oxidative reaction of uracils/thiouracil with 1,3-diarylpropenes is disclosed. It undergoes oxidative coupling, intramolecular cyclization, and dehydro-aromatization to provide multi-substituted pyrido[2,3-d]pyrimidines/thiopyrido[2,3-d]pyrimidines in moderate to excellent yields. It has the advantages of high atom economy, green terminal oxidant, and metal-free conditions. [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table ...
Source: Synthesis - September 27, 2023 Category: Chemistry Authors: Cheng, Dongping Xia, Hongshuang Gu, Huafang Wang, Yawei Li, Jing-Hua Xu, Xiaoliang Tags: paper Source Type: research
Linked PDF of Table of Contents
Synthesis 2023; 55: V- DOI: 10.1055/s-0040-1720092 Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents (Source: Synthesis)
Source: Synthesis - September 27, 2023 Category: Chemistry Tags: table of contents Source Type: research
Oxidative Cyclization Reactions Catalyzed by Designed Transition-Metal Complexes: A New Strategy for the Synthesis of Flavone, Quinolone, and Benzofuran Derivatives
Synthesis DOI: 10.1055/s-0042-1751489 An efficient and convenient synthetic protocol is reported for the synthesis of 2-phenyl-4H-chromen-4-one, 2-phenylquinolin-4(1H)-one, and 11H-benzofuro[3,2-b]chromen-11-one derivatives from 2′-hydroxychalcones, 2′-aminochalcones, and 3-hydroxyflavones, respectively, using transition-metal catalysts and TEMPO as an oxidizing agent. This catalytic heterocyclization approach involves in situ free-radical generation as phenoxyl radicals were detected by EPR spectroscopic study and H2O2 was formed. The present method has numerous advantages, such as high atom-economy, less hazardous sy...
Source: Synthesis - September 26, 2023 Category: Chemistry Authors: Singh, Apurva Singh, Sain Ghosh, Kaushik Ahmed, Naseem Tags: paper Source Type: research
Synform issue 2023/10
Synthesis 2023; 55: A167-A180 DOI: 10.1055/s-0040-1720611 Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents (Source: Synthesis)
Source: Synthesis - September 26, 2023 Category: Chemistry Authors: Zanda, Matteo Tags: Synform Source Type: research
Pd-Catalyzed Remote δ-C(sp2)–H Functionalization in Phenylalaninol: Expanding the Library of Phenylalaninols
We report the Pd(II)-catalyzed, picolinamide-directed δ-C(sp2)–H (ortho) functionalization of phenylalaninol scaffolds. Assembling of (ortho) δ-C–H arylated, alkylated, benzylated, alkenylated, brominated, and iodinated phenylalaninol scaffolds was accomplished. The δ-C(sp2)–H arylation reaction of phenylalaninol occurred under neat conditions. Hydrolysis of the picolinamide moiety and synthetic utility of the δ-C(sp2)–H arylated substrates were explored. We have also shown the preparation of some modified Matijin–Su (aurantiamide) derivatives using the bis δ-C–H (ortho) arylated phenylalaninol compounds o...
Source: Synthesis - September 25, 2023 Category: Chemistry Authors: Singh, Prabhakar Babu, Srinivasarao Arulananda Tags: paper Source Type: research
Asymmetric Hetero-Diels –Alder Reaction of 4-Phenyl-1,2,4-triazole-3,5-dione with 2,4-Dienyl Carboxylic Acids
Synthesis DOI: 10.1055/a-2131-0116 The enantioselective hetero-Diels–Alder reaction of the cyclic azo compound 4-phenyl-1,2,4-triazole-3,5-dione with 2,4-dienyl carboxylic acids was performed using tartaric acid ester as the chiral auxiliary. The corresponding cycloadducts were obtained with enantioselectivities of up to 76% ee. The cis-carboxylic acid produced could be converted into the corresponding cis- and trans-methyl esters by varying the reaction conditions. [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full text (Source: Synthesis)
Source: Synthesis - September 25, 2023 Category: Chemistry Authors: Sato, Yu Ukei, Takahiro Tsugeno, Hiromasa Suga, Takuya Soeta, Takahiro Ukaji, Yutaka Tags: paper Source Type: research
Cobalt-Catalyzed Enantioselective Alkynylation of Oxabicyclic Alkenes
Synthesis DOI: 10.1055/a-2152-0355 Efficient access to enantioenriched cyclic homopropargylic alcohols through an unprecedented cobalt-catalyzed asymmetric alkynylation of oxabicyclic alkenes has been developed. By using inexpensive cobalt salt/chiral bisphosphine ligand as the catalyst and easy-to-handle potassium alkynyltrifluoroborates as the nucleophile, synthetically valuable homopropargylic alcohols are obtained in moderate to good yields and high enantioselectivities. [...] Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, GermanyArticle in Thieme eJournals: Table of contents | Abstract | Full ...
Source: Synthesis - September 22, 2023 Category: Chemistry Authors: Wei, Lin-Wen Ma, Zhan-Cai Wang, Zhao-Qing Zhao, Yu Huang, Yuan Tags: paper Source Type: research
Synthesis and Immunological Evaluation of Escherichia coli O1-
Derived Oligosaccharide –Protein Conjugates toward Avian Pathogenic Escherichia coli O1 Vaccine Development
In this study, the first synthesis of the pentasaccharide repeating units of the O1B and O1C antigens was successfully achieved. The synthesis and immunological evaluation of their conjugates with bovine serum albumin (BSA) were conducted. Only the O1A-pentasaccharide structure is a glycotope candidate for APEC O1. Keyhole limpet hemocyanin (KLH)–O1A-pentasaccharide conjugate was also synthesized, and its immunogenicity was evaluated by the ELISA assay. The efficient production of antibodies capable of binding to both APEC O1 LPS and the O1A-pentasaccharide structure was observed, indicating that O1A-pentasaccharide is a...
Source: Synthesis - September 21, 2023 Category: Chemistry Authors: Seki, Katsunori Makikawa, Takumi Toshima, Kazunobu Takahashi, Daisuke Tags: special topic Source Type: research
