ReviewRSC medicinal chemistry2020
Recent progress toward the asymmetric synthesis of carbon-substituted piperazine pharmacophores and oxidative related heterocycles.
Review in RSC medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Stereoselective amino alcohol synthesis via chemoselective electrocatalytic radical cross-couplings.Nature chemistry · 2025Article
- Programmable Piperazine Synthesis via Organic Photoredox Catalysis.Journal of the American Chemical Society · 2024Article
- Chemoselective Diazine Dearomatization: The Catalytic Enantioselective Dearomatization of Pyrazine.Journal of the American Chemical Society · 2024Article
- Green Light Promoted Iridium(III)/Copper(I)-Catalyzed Addition of Alkynes to Aziridinoquinoxalines Through the Intermediacy of Azomethine Ylides.Angewandte Chemie (International ed. in English) · 2024Article
- Heterocyclic Merging of Stereochemically Diverse Chiral Piperazines and Morpholines with Indazoles.Chemistry (Weinheim an der Bergstrasse, Germany) · 2023Article
- Building Up a Piperazine Ring from a Primary Amino Group via Catalytic Reductive Cyclization of Dioximes.International journal of molecular sciences · 2023Article
- Synthesis and Biological Activity of Myricetin Derivatives Containing Pyrazole Piperazine Amide.International journal of molecular sciences · 2023Article
- Iridium-Catalyzed Regio- and Diastereoselective Synthesis of C-Substituted Piperazines.ACS catalysis · 2023Article
- Biopolymer-Based Nanosystems for siRNA Drug Delivery to Solid Tumors including Breast Cancer.Pharmaceutics · 2023Review
- Visible Light-Mediated, Diastereoselective Epimerization of Morpholines and Piperazines to More Stable Isomers.ACS catalysis · 2022Article
- Piperazine-derived lipid nanoparticles deliver mRNA to immune cells in vivo.Nature communications · 2022Article
- A Concise Synthetic Method for Constructing 3-Substituted Piperazine-2-Acetic Acid Esters from 1,2-Diamines.Molecules (Basel, Switzerland) · 2022Article
- Diketopiperazine Gels: New Horizons from the Self-Assembly of Cyclic Dipeptides.Molecules (Basel, Switzerland) · 2021Review
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Abstract
The important requirement for approval of a new drug, in case it happens to be chiral, is that both enantiomers of the drug should be studied in detail, which has led synthetic organic and medicinal chemists to focus their attention on the development of new methods for asymmetric synthesis especially of relevant saturated N-heterocycles. On the other hand, the piperazine ring, besides defining a major class of saturated N-heterocycles, has been classified as a privileged structure in medicinal chemistry, since it is more than frequently found in biologically active compounds including several marketed blockbuster drugs such as Glivec (imatinib) and Viagra (sildenafil). Indeed, 13 of the 200 best-selling small molecule drugs in 2012 contained a piperazine ring. Nevertheless, analysis of the piperazine substitution pattern reveals a lack of structural diversity, with almost every single drug in this category (83%) containing a substituent at both the N1- and N4-positions compared to a few drugs having a substituent at any other position (C2, C3, C5, and C6). Significant chemical space that is closely related to that known to be biologically relevant, therefore, remains unexplored. In order to explore this chemical space, efficient and asymmetric syntheses of carbon-substituted piperazines and related heterocycles must be designed and developed. Initial, recent efforts toward the implementation of this particular target are in fact the subject of this review.
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Registered trials
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