An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

Scholarly Works

• Shaikh, M. H.; Nagargoje, A. A.; Tamboli, Y.; Islam, I.; Shingate, B. B. A Concise Account of Synthetic Approaches to 1,2,3-Triazoles. Organic Preparations and Procedures International 2024, 1–33. doi:10.1080/00304948.2024.2334167
• Rana, S.; Shaw, R.; Pratap, R. Influence of steric hindrance on the 1,4- versus 1,6-Michael addition: synthesis of furans and pentasubstituted benzenes. Organic & biomolecular chemistry 2024. doi:10.1039/d4ob00686k
• Sveshnikova, A.; Oftadeh, O.; Hatzimanikatis, V. Designing pathways for bioproducing complex chemicals by combining tools for pathway extraction and ranking. Cold Spring Harbor Laboratory 2024. doi:10.1101/2024.06.10.598209
• Zhang, X.-H.; Wang, Z.-H.; Chen, Y.; Bai, M.; Wang, Z.-H.; Zhang, Y.-P.; You, Y.; Zhao, J.-Q.; Yuan, W.-C. Palladium-Catalyzed Cycloaddition Reactions of π-Allylpalladium 1,4-Dipoles with 1,3,5-Triazinanes: Access to Hexahydropyrimidines, 1,3-Oxazinanes, and 1,5-Diazocanes. The Journal of organic chemistry 2024, 89, 8363–8375. doi:10.1021/acs.joc.4c00128
• Zukic, E.; Mokos, D.; Weber, M.; Stix, N.; Ditrich, K.; Ferrario, V.; Müller, H.; Willrodt, C.; Gruber, K.; Daniel, B.; Kroutil, W. Biocatalytic Heteroaromatic Amide Formation in Water Enabled by a Catalytic Tetrad and Two Access Tunnels. ACS catalysis 2024, 14, 8913–8921. doi:10.1021/acscatal.4c01268
• Proos Vedin, N.; Escayola, S.; Radenković, S.; Solà, M.; Ottosson, H. The n,π* States of Heteroaromatics: When are They the Lowest Excited States and in What Way Can They Be Aromatic or Antiaromatic?. The journal of physical chemistry. A 2024, 128, 4493–4506. doi:10.1021/acs.jpca.4c02580
• Yang, Y.; Song, Q.; Sivaguru, P.; Liu, Z.; Shi, D.; Tian, T.; de Ruiter, G.; Bi, X. Controllable Skeletal and Peripheral Editing of Pyrroles with Vinylcarbenes. Angewandte Chemie 2024, 136. doi:10.1002/ange.202401359
• Yang, Y.; Song, Q.; Sivaguru, P.; Liu, Z.; Shi, D.; Tian, T.; de Ruiter, G.; Bi, X. Controllable Skeletal and Peripheral Editing of Pyrroles with Vinylcarbenes. Angewandte Chemie (International ed. in English) 2024, 63, e202401359. doi:10.1002/anie.202401359
• Rang, M.; Heinz, M.; Halkić, A.; Weber, M.; Dewhurst, R. D.; Rempel, A.; Härterich, M.; Holthausen, M. C.; Braunschweig, H. Trapping of a Terminal Intermediate in the Boron-Mediated Dinitrogen Reduction: Mono-, Tri-, and Tetrafunctionalized Hydrazines in Two Steps from N2. Journal of the American Chemical Society 2024. doi:10.1021/jacs.4c01818
• Thangavel, S. K.; Mohamed Kasim, M. S.; Rengan, R. Promoting the Anticancer Activity with Multidentate Furan-2-Carboxamide Functionalized Aroyl Thiourea Chelation in Binuclear Half-Sandwich Ruthenium(II) Complexes. Inorganic chemistry 2024, 63, 7520–7539. doi:10.1021/acs.inorgchem.4c01265
• Dehghany, M.; Pavaneli, G.; Kailing, J. W.; Duke, O. M.; Guzei, I. A.; Da Ros Montes D'Oca, C.; Fernández, I.; Schomaker, J. M. Tunable Divergent Reactivity of Aziridinium Ylides in the Synthesis of Complex Piperidines and Azetidines. ACS Catalysis 2024, 14, 5795–5803. doi:10.1021/acscatal.3c06173
• Kassem, A. F.; Moustafa, G. O.; Omran, M. M.; El-Sofany, W. I. Investigation on the pharmacological profile for new synthesized bis heterocyclic analogs containing nitrogen atom as anti-cancer therapy target. Journal of Molecular Structure 2024, 1312, 138450. doi:10.1016/j.molstruc.2024.138450
• Sunny, S.; Maingle, M.; Sheeba, L.; Pathan, F. R.; J., G. S.; Juloori, H.; Gadewar, S. G.; Seth, K. Cu(ii)-catalyzed 'in-water' N-arylation of electron-deficient NH-heterocycles. Green Chemistry 2024, 26, 3149–3158. doi:10.1039/d3gc05163c
• Bombonato, E.; Fasano, V.; Pecorari, D.; Fornasari, L.; Castagnini, F.; Marcaccio, M.; Ronchi, P. Electrochemical Synthesis of Unnatural Amino Acids Embedding 5- and 6-Membered Heteroaromatics. ACS omega 2024, 9, 13081. doi:10.1021/acsomega.3c09357
• Fan, J.; Zu, Y.; Zheng, Z.; Song, L.; Wang, Y.; Zhou, Z.; Liu, Y.; Xu, S. A silver-mediated radical process of β-keto sulfones for the synthesis of 2,3-diacyl furans. Organic & biomolecular chemistry 2024, 22, 1770–1774. doi:10.1039/d3ob02079g
• Singh, K.; Gupta, J. K.; Shah, K.; Saha, S.; Babu, M. A.; Kumar, S.; Agrawal, M. Harnessing the Pyrazine Moiety for Potent Anti-inflammatory Activity: A Comprehensive Review. Current Organic Chemistry 2024, 28, 176–184. doi:10.2174/0113852728279887240109110636
• Tsurugi, H.; Akiyama, T.; Frye, C. W.; Kakiuchi, Y.; Mashima, K.; Tonks, I. A. Evaluation of Tungsten Catalysis among Early Transition Metals for N-Aryl-2,3,4,5-tetraarylpyrrole Synthesis: Modular Access to N-Doped π-Conjugated Material Precursors. Inorganic chemistry 2024, 63, 3037–3046. doi:10.1021/acs.inorgchem.3c03858
• Gao, P.; Wang, Z.; Chang, R.; Li, W.; Zhao, Z.; Fu, D.; Liu, Q. Ruthenium/HI-catalyzed direct hydromethylation of indoles and quinolines in DME. New Journal of Chemistry 2024, 48, 1227–1232. doi:10.1039/d3nj03341d
• Natarajan, P.; Kanchithalaivan, S.; Chatterjee, A.; Peruncheralathan, S. Organocatalytic Chemoselective C4‐Benzylation of 5‐Aminopyrazoles. Asian Journal of Organic Chemistry 2024, 13. doi:10.1002/ajoc.202300628
• Garg, A.; Bhalla, A. Environmental-benign pathways for the synthesis of medicinally relevant heterocycles. Green Approaches in Medicinal Chemistry for Sustainable Drug Design; Elsevier, 2024; pp 361–396. doi:10.1016/b978-0-443-16166-7.00023-2

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