Multicomponent Reactions in Medicinal Chemistry

Wang, Zefeng; Dömling, Alexander

doi:10.1002/9783527832439.ch3

Cited by 10 publications

(7 citation statements)

References 150 publications

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“…Even though the classical IMCRs are not suited for generating heterocyclic compounds, new variations of the Passerini three-component reaction [ 48 , 57 ], Ugi three- and four-component reaction (U-4CR) [ 58 , 59 ], van Leusen reaction [ 60 ] and Groebke–Blackburn–Bienaymé reaction (GBBR) [ 61 , 62 , 63 , 64 ] have been explored and, indeed, IMCRs are leading today’s MCR chemistry [ 65 ]. For further information on isocyanide chemistry, the reader is directed toward further comprehensive review articles from Prof. Heravi’s group [ 66 , 67 , 68 , 69 , 70 ], Prof. Dömling’s group [ 71 , 72 , 73 , 74 , 75 , 76 , 77 , 78 , 79 , 80 , 81 , 82 ] and other extensive publications [ 83 , 84 , 85 , 86 , 87 , 88 , 89 , 90 , 91 , 92 , 93 , 94 , 95 ].…”

Section: Introduction: Multicomponent Reactionsmentioning

confidence: 99%

“…For the generation of a diverse scaffold, other NIMCRs implemented are, namely, Pavarov-3CR, Dobener-3CR, Betti-3CR, and Petasis-3CR ( Figure 4 ). For further information on NIMCRs chemistry, the reader is directed toward comprehensive review articles and other very interesting recent publications [ 89 , 90 , 92 , 93 , 103 , 104 , 105 , 106 , 107 , 108 , 109 , 110 , 111 , 112 , 113 ].…”

Section: Introduction: Multicomponent Reactionsmentioning

confidence: 99%

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Multicomponent Reaction-Assisted Drug Discovery: A Time- and Cost-Effective Green Approach Speeding Up Identification and Optimization of Anticancer Drugs

Graziano

Stefanachi

Contino

et al. 2023

IJMS

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Multicomponent reactions (MCRs) have emerged as a powerful strategy in synthetic organic chemistry due to their widespread applications in drug discovery and development. MCRs are flexible transformations in which three or more substrates react to form structurally complex products with high atomic efficiency. They are being increasingly appreciated as a highly exploratory and evolutionary tool by the medicinal chemistry community, opening the door to more sustainable, cost-effective and rapid synthesis of biologically active molecules. In recent years, MCR-based synthetic strategies have found extensive application in the field of drug discovery, and several anticancer drugs have been synthesized through MCRs. In this review, we present an overview of representative and recent literature examples documenting different approaches and applications of MCRs in the development of new anticancer drugs.

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Section: Introduction: Multicomponent Reactionsmentioning

confidence: 99%

Section: Introduction: Multicomponent Reactionsmentioning

confidence: 99%

Multicomponent Reaction-Assisted Drug Discovery: A Time- and Cost-Effective Green Approach Speeding Up Identification and Optimization of Anticancer Drugs

Graziano

Stefanachi

Contino

et al. 2023

IJMS

View full text Add to dashboard Cite

show abstract

“…The development of MCRs continues at a considerable pace in reaction discovery, organic synthesis, etc., and their application in medicinal chemistry is gaining momentum. The implementation of this methodology is having a deep impact on hit finding, greatly helping the production of combinatorial libraries (key for SAR studies), hit-to-lead (H2L) stage, lead optimization and large-scale preparation of complex medicines [ 16 , 17 , 18 ].…”

Section: Introductionmentioning

confidence: 99%

Heterocycle-Based Multicomponent Reactions in Drug Discovery: From Hit Finding to Rational Design

et al. 2022

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In the context of the structural complexity necessary for a molecule to selectively display a therapeutical action and the requirements for suitable pharmacokinetics, a robust synthetic approach is essential. Typically, thousands of relatively similar compounds should be prepared along the drug discovery process. In this respect, heterocycle-based multicomponent reactions offer advantages over traditional stepwise sequences in terms of synthetic economy, as well as the fast access to chemsets to study the structure activity relationships, the fine tuning of properties, and the preparation of larger amounts for preclinical phases. In this account, we briefly summarize the scientific methodology backing the research line followed by the group. We comment on the main results, clustered according to the targets and, finally, in the conclusion section, we offer a general appraisal of the situation and some perspectives regarding future directions in academic and private research.

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“…These multicomponent strategies provide great molecular diversity in a single step and in a highly efficient manner [ 1 , 2 , 3 ]. The utility of these processes has been confirmed by the synthesis of a large number of compounds with remarkable biological activity [ 4 , 5 ].…”

Section: Introductionmentioning

confidence: 99%

Piperidine-Iodine as Efficient Dual Catalyst for the One-Pot, Three-Component Synthesis of Coumarin-3-Carboxamides

et al. 2022

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A simple and efficient one-pot, three-component synthetic method for the preparation of coumarin-3-carboxamides was carried out by the reaction of salicylaldehyde, aliphatic primary/secondary amines, and diethylmalonate. The protocol employs piperidine-iodine as a dual system catalyst and ethanol, a green solvent. The main advantages of this approach are that it is a metal-free and clean reaction, has low catalyst loading, and requires no tedious workup.

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Multicomponent Reactions in Medicinal Chemistry

Cited by 10 publications

References 150 publications

Multicomponent Reaction-Assisted Drug Discovery: A Time- and Cost-Effective Green Approach Speeding Up Identification and Optimization of Anticancer Drugs

Multicomponent Reaction-Assisted Drug Discovery: A Time- and Cost-Effective Green Approach Speeding Up Identification and Optimization of Anticancer Drugs

Heterocycle-Based Multicomponent Reactions in Drug Discovery: From Hit Finding to Rational Design

Piperidine-Iodine as Efficient Dual Catalyst for the One-Pot, Three-Component Synthesis of Coumarin-3-Carboxamides

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