Kinzel, Olaf’s team published research in Bioorganic & Medicinal Chemistry Letters in 2016 | CAS: 18621-18-6

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.COA of Formula: C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

In 2016,Kinzel, Olaf; Steeneck, Christoph; Schlueter, Thomas; Schulz, Andreas; Gege, Christian; Hahn, Ulrike; Hambruch, Eva; Hornberger, Martin; Spalwisz, Adriana; Frick, Katharina; Perovic-Ottstadt, Sanja; Deuschle, Ulrich; Burnet, Michael; Kremoser, Claus published 《Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties》.Bioorganic & Medicinal Chemistry Letters published the findings.COA of Formula: C3H8ClNO The information in the text is summarized as follows:

Several isoxazole-containing series of FXR agonists have been published over the last 15 years, subsequent to the prototypical amphiphilic ‘hammerhead’-type structure that was originally laid out by GW4064, the first potent synthetic FXR agonist. A set of novel compounds where the hammerhead is connected to the terminal carboxylic acid-bearing aryl or heteroaryl moiety by either a cyclopropyl, a hydroxycyclobutyl or a hydroxyazetidinyl linker was synthesized in order to improve upon the ADME properties of such isoxazoles. The resulting compounds all demonstrated high potencies at the target receptor FXR but with considerable differences in their physicochem. and in vivo profiles. The structure-activity relationships for key chem. features that have a major impact on the in vivo pharmacol. of this series are discussed. The experimental part of the paper was very detailed, including the reaction process of Azetidin-3-ol hydrochloride(cas: 18621-18-6COA of Formula: C3H8ClNO)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.COA of Formula: C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

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