1451998-23-4Relevant academic research and scientific papers
Chemodivergent and Stereoselective Access to Fused Isoxazoline Azetidines and Thietanes through [3 + 2]-Cycloadditions
Baumann, Andreas N.,Reiners, Felix,Juli, Thomas,Didier, Dorian
, p. 6736 - 6740 (2018)
By combining efficient methodologies for the preparation of substituted azetines and thietes with a highly regio- and diastereoselective [3 + 2]-cycloaddition, a straightforward pathway for the synthesis of fused isoxazoline azetidines and thietanes has been designed. With minimal steps and starting from commercial sources, a new library of elaborated architectures was synthesized opening up a new class of molecules with large potential in pharmacology. Finally, a retro [2 + 2]-cycloaddition leading to substituted isoxazoles is described.
Methods for the Synthesis of Substituted Azetines
Baumann, Andreas N.,Eisold, Michael,Music, Arif,Haas, Geoffrey,Kiw, Yu Min,Didier, Dorian
, p. 5681 - 5684 (2017)
Spurred on by the recent emerging interest from the chemical community for unsaturated four-membered heterocycles, an unprecedented approach to nitrogen-containing four-membered rings has been designed. 3,4-Disubstituted 2-azetines were synthesized from c
Regiodivergent Stereoselective Access to Fused Alkylideneazetidines
Music, Arif,Baumann, Andreas N.,Eisold, Michael,Didier, Dorian
, p. 783 - 792 (2018)
Following recent advances in the generalization and simplification of 2H-azetine synthesis, a regiodivergent approach to fused 2- and 3-alkylideneazetines was designed via the intermediate formation of unprecedented vinylazetine structures. Concise sequen
Stereoselective Access to Azetidine-Based α-Amino Acids and Applications to Small Peptide Synthesis
Didier, Dorian,Joseph, Emanuel,Ni?l, Benedikt,Reiners, Felix
, p. 8533 - 8537 (2020/11/18)
Non-natural azetidine-based amino acids (Aze) present interesting features in protein engineering. A simple organometallic route toward unsaturated carboxylic acid precursors is presented. Subsequent metal-catalyzed asymmetric reduction allowed for the sy
SUBSTITUTED 5-AMINOTHIENO[2,3-C]PYRIDAZINE-6-CARBOXAMIDE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4
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, (2013/09/12)
In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6- carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
