The Versatility of the Roskamp Homologation in Synthesis

Modern organic synthesis continues to benefit from the flexibility of α-diazo carbonyl intermediates. In the context of homologation processes, the Roskamp reaction—first introduced in 1989—has become a valuable tool due to its selectivity and mild condition reactions for accessing important synthon...

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Main Authors: Margherita Miele, Aljoša Smajić, Vittorio Pace
Format: Article
Language:English
Published: MDPI AG 2025-03-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/30/6/1192
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author Margherita Miele
Aljoša Smajić
Vittorio Pace
author_facet Margherita Miele
Aljoša Smajić
Vittorio Pace
author_sort Margherita Miele
collection DOAJ
description Modern organic synthesis continues to benefit from the flexibility of α-diazo carbonyl intermediates. In the context of homologation processes, the Roskamp reaction—first introduced in 1989—has become a valuable tool due to its selectivity and mild condition reactions for accessing important synthons amenable to further functionalization as β-keto esters. The fine-tuning of reaction parameters—including the nature of Lewis acids, solvents, and temperature—has enabled the development of catalyzed continuous-flow methodologies, as well as a series of asymmetric variants characterized by high transformation rates, excellent stereocontrol, and formidable chemoselectivity. This review aims to emphasize the attractive features of the Roskamp reaction and its applicability for addressing challenging homologation processes.
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spelling doaj-art-397a6b57be1f4439b2b105f609aa16152025-08-20T02:42:22ZengMDPI AGMolecules1420-30492025-03-01306119210.3390/molecules30061192The Versatility of the Roskamp Homologation in SynthesisMargherita Miele0Aljoša Smajić1Vittorio Pace2Department of Chemistry, University of Turin, Via P. Giuria 7, 10125 Turin, ItalyDivision of Pharmaceutical Chemistry, Department of Pharmaceutical Sciences, University of Vienna, Josef-Holaubek-Platz 2, A-1090 Vienna, AustriaDepartment of Chemistry, University of Turin, Via P. Giuria 7, 10125 Turin, ItalyModern organic synthesis continues to benefit from the flexibility of α-diazo carbonyl intermediates. In the context of homologation processes, the Roskamp reaction—first introduced in 1989—has become a valuable tool due to its selectivity and mild condition reactions for accessing important synthons amenable to further functionalization as β-keto esters. The fine-tuning of reaction parameters—including the nature of Lewis acids, solvents, and temperature—has enabled the development of catalyzed continuous-flow methodologies, as well as a series of asymmetric variants characterized by high transformation rates, excellent stereocontrol, and formidable chemoselectivity. This review aims to emphasize the attractive features of the Roskamp reaction and its applicability for addressing challenging homologation processes.https://www.mdpi.com/1420-3049/30/6/1192homologationRoskamp reactionasymmetric reactionα-diazocarbonyl compoundsWeinreb amidesα-silyl ketones
spellingShingle Margherita Miele
Aljoša Smajić
Vittorio Pace
The Versatility of the Roskamp Homologation in Synthesis
Molecules
homologation
Roskamp reaction
asymmetric reaction
α-diazocarbonyl compounds
Weinreb amides
α-silyl ketones
title The Versatility of the Roskamp Homologation in Synthesis
title_full The Versatility of the Roskamp Homologation in Synthesis
title_fullStr The Versatility of the Roskamp Homologation in Synthesis
title_full_unstemmed The Versatility of the Roskamp Homologation in Synthesis
title_short The Versatility of the Roskamp Homologation in Synthesis
title_sort versatility of the roskamp homologation in synthesis
topic homologation
Roskamp reaction
asymmetric reaction
α-diazocarbonyl compounds
Weinreb amides
α-silyl ketones
url https://www.mdpi.com/1420-3049/30/6/1192
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