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Keywords = Asinger reaction

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42 pages, 13456 KB  
Review
Multicomponent Reactions for the Synthesis of Active Pharmaceutical Ingredients
by Ángel Cores, José Clerigué, Emmanuel Orocio-Rodríguez and J. Carlos Menéndez
Pharmaceuticals 2022, 15(8), 1009; https://doi.org/10.3390/ph15081009 - 17 Aug 2022
Cited by 80 | Viewed by 16479
Abstract
Multicomponent reactions 9i.e., those that engage three or more starting materials to form a product that contains significant fragments of all of them), have been widely employed in the construction of compound libraries, especially in the context of diversity-oriented synthesis. While relatively less [...] Read more.
Multicomponent reactions 9i.e., those that engage three or more starting materials to form a product that contains significant fragments of all of them), have been widely employed in the construction of compound libraries, especially in the context of diversity-oriented synthesis. While relatively less exploited, their use in target-oriented synthesis offers significant advantages in terms of synthetic efficiency. This review provides a critical summary of the use of multicomponent reactions for the preparation of active pharmaceutical principles. Full article
(This article belongs to the Special Issue Multicomponent and Domino Reactions in Drug Discovery)
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6 pages, 232 KB  
Proceeding Paper
Microwave-Assisted Asinger Synthesis of Thiazolines
by Raúl Eduardo Gordillo-Cruz, Liliana Gonzalez-Reyes, Milton Coporo-Reyes, Nieves Zavala-Segovia, Bernardo A. Frontana-Uribe, Marco A. García-Eleno, M. V. Basavanag Unnamatla and Erick Cuevas-Yañez
Chem. Proc. 2021, 3(1), 27; https://doi.org/10.3390/ecsoc-24-08316 - 14 Nov 2020
Cited by 1 | Viewed by 2378
Abstract
An array of 2,4-disubstituted thiazolines was obtained through Asinger reaction approach from the straightforward treatment of diverse aldehydes/ketones with 1-mercaptopropan-2-one, in the presence of NH3 assisted by microwave irradiation, displaying similar and sometimes higher yields, as well as shorter reaction times that [...] Read more.
An array of 2,4-disubstituted thiazolines was obtained through Asinger reaction approach from the straightforward treatment of diverse aldehydes/ketones with 1-mercaptopropan-2-one, in the presence of NH3 assisted by microwave irradiation, displaying similar and sometimes higher yields, as well as shorter reaction times that traditional Asinger reaction conditions at room and lower temperatures. Full article
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10 pages, 1830 KB  
Article
Merging Heterocyclic Chemistry and Biocatalysis in One-Pot Processes through Compartmentalization of the Reaction Steps
by Nadine Zumbrägel and Harald Gröger
Bioengineering 2018, 5(3), 60; https://doi.org/10.3390/bioengineering5030060 - 1 Aug 2018
Cited by 19 | Viewed by 7269
Abstract
A proof of concept for a one-pot process merging a heterocycle formation by a classical chemical approach at basic conditions with a biocatalytic reduction, running at neutral pH conditions, is reported. A crucial component for this process is the compartmentalization of the single [...] Read more.
A proof of concept for a one-pot process merging a heterocycle formation by a classical chemical approach at basic conditions with a biocatalytic reduction, running at neutral pH conditions, is reported. A crucial component for this process is the compartmentalization of the single reactions by the use of polydimethylsiloxane thimbles. This process was applied successfully towards an asymmetric synthesis of (S)-2,2,3-trimethyl-1-thia-4-azaspiro[4.4]nonane, leading to excellent enantioselectivities of 99% enantiomeric excess (ee). Full article
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