The Ugi reaction as the green alternative towards active pharmaceutical ingredients

Tetrahedron Green Chem, Journal Year: 2024, Volume and Issue: 3, P. 100044 - 100044

Published: May 23, 2024

Α sustainable access to therapeutics is today imperative. More than ever, synthetic organic chemistry has embrace all aspects of green chemistry. The utility multicomponent reactions especially the Ugi reaction an established approach in drug discovery. Their diversity, speed and effectiveness, combined with their compatibility principles, render this type very often alternative multistep linear pathways active pharmaceutical ingredients. This critical review compares metrics, such as E-factor (environmental factor), AE (atom economy) PMI (process mass intensity) factors, industrial MCR syntheses six well-known commercial drugs.

Language: Английский

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Heteroannulations of cyanoacetamide-based MCR scaffolds utilizing formamide

Beilstein Journal of Organic Chemistry, Journal Year: 2025, Volume and Issue: 21, P. 217 - 225

Published: Jan. 24, 2025

C1 chemistry has a central role in the efficient utilization of single-carbon molecules, contributing significantly to sustainability, innovation and economic growth across various sectors. In this study, we present an rapid method for synthesizing variety heteroannulated pyrimidones using cyanoacetamide-based multicomponent reaction (MCR) chemistry. By utilizing specific MCR-based scaffolds as precursors employing abundant inexpensive formamide feedstock under neat conditions, were able efficiently access substituted thieno-, quinolino- indolopyrimidones without need column chromatography. Further, single-crystal X-ray structure was obtained, revealing certain geometrical features.

Language: Английский

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Directed Regioselective Arylation of Imidazo[1,2-a]pyridine-3-carboxamides using Rh(III) catalysis.

Organic & Biomolecular Chemistry, Journal Year: 2024, Volume and Issue: 22(35), P. 7121 - 7127

Published: Jan. 1, 2024

We introduced, for the first time, N -methoxyamide directed proximal C–H bond activation of imidazo[1,2- a ]pyridines C(sp 2 )–C(sp ) formation via transition metal catalysed approach to obtain C-5 arylated ]pyridines.

Language: Английский

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Generation of multimillion chemical space based on the parallel Groebke–Blackburn–Bienaymé reaction

Beilstein Journal of Organic Chemistry, Journal Year: 2024, Volume and Issue: 20, P. 1604 - 1613

Published: July 16, 2024

Parallel Groebke-Blackburn-Bienaymé reaction was evaluated as a source of multimillion chemically accessible chemical space. Two most popular classical protocols involving the use Sc(OTf)

Language: Английский

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MCR-based C1 heteroannulations

Published: Aug. 14, 2024

C1 chemistry has a central role in efficiently utilizing single-carbon-molecules contributing significantly to sustainability, innovation and economic growth across various sectors. In this study, we present an efficient rapid method for synthesizing variety of heteropyrimidones using cyanoacetamide-based multicomponent reaction (MCR) chemistry. By employing the abundant inexpensive formamide as feedstock under neat conditions, were able access substituted thieno-, quinolino- indolo-pyrimidones one-pot process. A single crystal structure been obtained revealing certain geometrical features.

Language: Английский

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Synthesis of imidazo[2,1-b]thiazol-5-amines using Groebke–Blackburn–Bienaymé multicomponent reaction (microreview)

Chemistry of Heterocyclic Compounds, Journal Year: 2024, Volume and Issue: 60(7-8), P. 339 - 341

Published: Aug. 1, 2024

Language: Английский

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Five-membered ring systems: With more than 1 N atom

Progress in heterocyclic chemistry, Journal Year: 2024, Volume and Issue: unknown, P. 211 - 257

Published: Jan. 1, 2024

Language: Английский

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