Ikeda, Shuhei team published research in Journal of Medicinal Chemistry in 2021 | 141699-55-0

141699-55-0, Tert-butyl 3-hydroxyazetidine-1-carboxylate is a useful research compound. Its molecular formula is C8H15NO3 and its molecular weight is 173.21 g/mol. The purity is usually 95%.

Tert-butyl 3-hydroxyazetidine-1-carboxylate has been shown to be a good substrate for the preparation of N-protected amino alcohols and amines by the process of reductive amination. In this synthesis, tert-butyl azetidinium chloride is used as a catalyst in the reaction with sodium hydroxide. The tert-butyl group can be removed using ammonium hydroxide in the presence of a base such as triethylamine. This reaction can be performed on a large scale, making it useful in the manufacture of pharmaceuticals. The efficiency and solubility of this process make it suitable for use as an introduction to other processes involving N-protected amino alcohols or amines., Reference of 141699-55-0

Simple alcohols are found widely in nature. Ethanol is the most prominent because it is the product of fermentation, a major energy-producing pathway. 141699-55-0, formula is C8H15NO3, Other simple alcohols, chiefly fusel alcohols, are formed in only trace amounts. More complex alcohols however are pervasive, as manifested in sugars, some amino acids, and fatty acids. , Reference of 141699-55-0

Ikeda, Shuhei;Sugiyama, Hideyuki;Tokuhara, Hidekazu;Murakami, Masataka;Nakamura, Minoru;Oguro, Yuya;Aida, Jumpei;Morishita, Nao;Sogabe, Satoshi;Dougan, Douglas R.;Gay, Sean C.;Qin, Ling;Arimura, Naoto;Takahashi, Yasuko;Sasaki, Masako;Kamada, Yusuke;Aoyama, Kazunobu;Kimoto, Kouya;Kamata, Makoto research published 《 Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl Moiety》, the research content is summarized as follows. The therapeutic potential of monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases has attracted attention worldwide. However, the availability of reversible-type inhibitor is still limited to clarify the pharmacol. effect. Herein, we report the discovery of novel spiro chem. series as potent and reversible MAGL inhibitors with a different binding mode to MAGL using Arg57 and His121. Starting from hit compound 1 and its co-crystal structure with MAGL, structure-based drug discovery (SBDD) approach enabled us to generate various spiro scaffolds like 2a (azetidine-lactam), 2b (cyclobutane-lactam), and 2d (cyclobutane-carbamate) as novel bioisosteres of 3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl moiety in 1 with higher lipophilic ligand efficiency (LLE). Optimization of the left hand side afforded 4f (I) as a promising reversible MAGL inhibitor, which showed potent in vitro MAGL inhibitory activity (IC50 6.2 nM), good oral absorption, blood-brain barrier penetration, and significant pharmacodynamic changes (2-arachidonoylglycerol increase and arachidonic acid decrease) at 0.3-10 mg/kg, po. in mice.

141699-55-0, Tert-butyl 3-hydroxyazetidine-1-carboxylate is a useful research compound. Its molecular formula is C8H15NO3 and its molecular weight is 173.21 g/mol. The purity is usually 95%.

Tert-butyl 3-hydroxyazetidine-1-carboxylate has been shown to be a good substrate for the preparation of N-protected amino alcohols and amines by the process of reductive amination. In this synthesis, tert-butyl azetidinium chloride is used as a catalyst in the reaction with sodium hydroxide. The tert-butyl group can be removed using ammonium hydroxide in the presence of a base such as triethylamine. This reaction can be performed on a large scale, making it useful in the manufacture of pharmaceuticals. The efficiency and solubility of this process make it suitable for use as an introduction to other processes involving N-protected amino alcohols or amines., Reference of 141699-55-0

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts