Multicomponent Reactions for the Synthesis of Bioactive Compounds: A Review

Graebin, Cedric Stephan; Ribeiro, Felipe Vitório; Rogerio, Kamilla Rodrigues; Kümmerle, Arthur Eugen

doi:10.2174/1570179416666190718153703

Cited by 155 publications

(70 citation statements)

References 184 publications

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“…The varied activity of DHPMs, combined with their synthetic accessibility and the possibility to rapidly assemble diverse substituents on the heterocyclic scaffold in a single multicomponent reaction, make the Biginelli reaction an attractive approach for the discovery of new biological activities. Multicomponent reactions, in particular, show great promise in the discovery of small molecule protease inhibitors possessing better pharmacological properties than peptidomimetic inhibitors [ 14 , 15 , 16 ].…”

Section: Introductionmentioning

confidence: 99%

One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues

et al. 2020

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A library of dihydropyrimidinones was synthesized via a “one-pot” three component Biginelli reaction using different aldehydes in combination with β-dicarbonyl compounds and urea. Selected 2-thiooxo and 2-imino analogs were also obtained with the Biginelli reaction from thiourea and guanidine hydrochloride, respectively. The products were screened in vitro for their β-secretase inhibitory activity. The majority of the compounds resulted to be active, with IC50 in the range 100 nM–50 μM.

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Section: Introductionmentioning

confidence: 99%

One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues

et al. 2020

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“…Multicomponent reactions reflect also the state of the art in chemical control since generally C-C and C-X (X = heteroatom) bonds are formed in one single step. For recent interesting applications of mechanochemistry in multicomponent reactions see references [ 78 , 79 , 80 , 81 , 82 , 83 , 84 , 85 , 86 , 87 ].…”

Section: Mechanochemistrymentioning

confidence: 99%

Novel Methodologies for Chemical Activation in Organic Synthesis under Solvent-Free Reaction Conditions

Avila‐Ortiz

Juaristi

2020

Molecules

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One central challenge for XXI century chemists is the development of sustainable processes that do not represent a risk either to humanity or to the environment. In this regard, the search for more efficient and clean alternatives to achieve the chemical activation of molecules involved in chemical transformations has played a prominent role in recent years. The use of microwave or UV-Vis light irradiation, and mechanochemical activation is already widespread in many laboratories. Nevertheless, an additional condition to achieve “green” processes comes from the point of view of so-called atom economy. The removal of solvents from chemical reactions generally leads to cleaner, more efficient and more economical processes. This review presents several illustrative applications of the use of sustainable protocols in the synthesis of organic compounds under solvent-free reaction conditions.

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“…[ 27–28 ] Moreover, the MCRs approach is widely used for the synthesis of various heterocyclic systems. [ 29–32 ]…”

Section: Introductionmentioning

confidence: 99%

Multicomponent one‐pot synthesis of novel imidazole‐2‐thione derivatives containing allomaltol fragment

Komogortsev

Melekhina

Lichitsky

et al. 2021

Journal of Heterocyclic Chem

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A convenient method for the synthesis of novel imidazole‐2‐thione derivatives containing allomaltol fragment was elaborated. This approach includes one‐pot multicomponent reaction of allomaltol, arylglyoxals, primary amines followed by addition of alkyl or aryl isothiocyanates. It was shown that the key intermediates of the studied process are substituted α‐aminoketones and the corresponding imidazolidine‐2‐thione. The advantages of this synthesis are mild reaction conditions, atom economy, and easy workup procedure, which can avoid chromatographic purifications. The structures of an intermediate imidazolidine‐2‐thione and one of the final imidazole‐2‐thiones were determined by X‐ray diffraction.

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Multicomponent Reactions for the Synthesis of Bioactive Compounds: A Review

Cited by 155 publications

References 184 publications

One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues

One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues

Novel Methodologies for Chemical Activation in Organic Synthesis under Solvent-Free Reaction Conditions

Multicomponent one‐pot synthesis of novel imidazole‐2‐thione derivatives containing allomaltol fragment

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