Domino reactions in the synthesis of heterocyclic natural products and analogs

LF Tietze, N Rackelmann - Pure and Applied Chemistry, 2004 - degruyter.com
Domino reactions are defined as processes of two or more bond-forming reactions under
identical conditions, in which the subsequent transformation takes place at the functionalities …

Enantioselective Total Syntheses of the Ipecacuanha Alkaloid Emetine, the Alangium Alkaloid Tubulosine and a Novel Benzoquinolizidine Alkaloid by Using a …

LF Tietze, N Rackelmann… - Chemistry–A European …, 2004 - Wiley Online Library
The first enantioselective syntheses of the Ipecacuanha alkaloid emetine (1) and the
Alangium alkaloid tubulosine (2) is described employing a domino Knoevenagel/hetero‐Diels–…

Stereochemical and Mechanistic Investigations of a Palladium‐Catalyzed Annulation of Secondary Alkyl Iodides

A Rudolph, N Rackelmann, M Lautens - Angewandte Chemie, 2007 - Wiley Online Library
Transition-metal-catalyzed reactions are widely used as valuable tools for carbon–carbon
bond formation.[1] Whereas palladium and nickel have classically occupied a central role in …

Photoredox‐Mediated Hydrogen Isotope Exchange Reactions of Amino‐Acids, Peptides, and Peptide‐Derived Drugs

…, H Mora‐Radó, N Rackelmann… - … A European Journal, 2020 - Wiley Online Library
Hydrogen isotopically labelled compounds are essential diagnostic tools in drug research
and development, as they provide vital information about the biological metabolism of drug …

Application of secondary alkyl halides to a domino aryl alkylation reaction for the synthesis of aromatic heterocycles

A Rudolph, N Rackelmann… - The Journal of …, 2009 - ACS Publications
A palladium-catalyzed, norbornene-mediated ortho-alkylation reaction of aryl iodides with
secondary alkyl halides is described. Intermolecular or intramolecular ortho-alkylation …

Design, synthesis, and pharmacological evaluation of potent positive allosteric modulators of the glucagon-like peptide-1 receptor (GLP-1R)

…, H Mors, M Podeschwa, N Rackelmann… - Journal of Medicinal …, 2019 - ACS Publications
The therapeutic success of peptidic GLP-1 receptor agonists for treatment of type 2 diabetes
mellitus (T2DM) motivated our search for orally bioavailable small molecules that can …

The Domino‐Knoevenagel‐Hetero‐Diels–Alder Reaction and Related Transformations

LF Tietze, N Rackelmann - Multicomponent reactions, 2005 - Wiley Online Library
The development of novel materials and the search for new bioactive compounds, such as
natural products and analogues, drugs, diagnostics and agrochemicals, in academic and …

Discovery and Optimization of 1-Phenoxy-2-aminoindanes as Potent, Selective, and Orally Bioavailable Inhibitors of the Na+/H+ Exchanger Type 3 (NHE3)

N Rackelmann, H Matter, H Englert… - Journal of Medicinal …, 2016 - ACS Publications
The design, synthesis, and structure–activity relationship of 1-phenoxy-2-aminoindanes as
inhibitors of the Na + /H + exchanger type 3 (NHE3) are described based on a hit from high-…

SAR340835, a novel selective Na+/Ca2+ exchanger inhibitor, improves cardiac function and restores sympathovagal balance in heart failure

…, K Wirth, H Gögelein, P Arndt, N Rackelmann… - … of Pharmacology and …, 2021 - ASPET
In failing hearts, Na + /Ca 2+ exchanger (NCX) overactivity contributes to Ca 2+ depletion,
leading to contractile dysfunction. Inhibition of NCX is expected to normalize Ca 2+ …

Enantioselective synthesis of Epi-emetine analogues: Control of the facial selectivity in a three-component domino Knoevenagel-Hetero-Diels-Alder reaction

LF Tietze, N Rackelmann - Zeitschrift für Naturforschung B, 2004 - degruyter.com
The domino Knoevenagel-hetero-Diels-Alder reaction of the aldehyde rac-8, Meldrum’s acid
2 and enol ether 3 leads to the cycloadduct rac-17 as the main product which in a second …