[EN] MUSCARINIC ACETYLCHOLINE M1 RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DES RÉCEPTEURS MUSCARINIQUES DE L'ACÉTYLCHOLINE M1
申请人:PIPELINE THERAPEUTICS INC
公开号:WO2021071843A1
公开(公告)日:2021-04-15
Provided herein, inter alia, are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic 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.
Manganese-catalyzed ring-opening carbonylation of cyclobutanol derivatives
作者:Tim Meyer、Zhiping Yin、Xiao-Feng Wu
DOI:10.1016/j.tetlet.2019.02.028
日期:2019.3
Herein, we report a manganese-catalyzed ring-opening carbonylation of cyclobutanol derivatives through cyclic CC bond cleavage. The reaction happens via a radical-mediated pathway to selectively generate 1,5-ketoesters. A variety of substrates with substituents on the aromatic ring reacted with linear alcohols of different chain lengths. Obtained aliphatic esters are very attractive since they are
Silver-Catalyzed Ring-Opening Strategy for the Synthesis of β- and γ-Fluorinated Ketones
作者:Huijun Zhao、Xuefeng Fan、Jiajia Yu、Chen Zhu
DOI:10.1021/jacs.5b00939
日期:2015.3.18
A regioselective synthesis of β- and γ-fluorinated ketones via silver-catalyzed ring opening is described. A variety of β- and γ-fluorinated ketones are efficiently prepared, respectively, from tertiary cyclopropanol and cyclobutanol precursors, providing a straightforward approach for the introduction of a fluorine atom into complex molecules. Preliminary mechanistic studies suggest that a radical-mediated
描述了通过银催化开环的 β- 和 γ-氟化酮的区域选择性合成。各种β-和γ-氟化酮分别由叔环丙醇和环丁醇前体有效制备,为将氟原子引入复杂分子提供了一种直接的方法。初步机理研究表明,涉及自由基介导的连续 CC 键裂解和 CF 键形成途径。
Tandem Oxidative Ring-Opening/Cyclization Reaction in Seconds in Open Atmosphere for the Synthesis of 1-Tetralones in Water–Acetonitrile
作者:Jingxian Fang、Lesong Li、Chu Yang、Jinping Chen、Guo-Jun Deng、Hang Gong
DOI:10.1021/acs.orglett.8b03246
日期:2018.11.16
A mild and practical tandem oxidative ring-opening/cyclization reaction mediated by Ce4+ for the synthesis of 1-tetralones is presented. This rapid transformation was completed within 30 s and conducted in an open reactor at 0 °C in a water–acetonitrile mixture. Various cyclobutanol derivatives are transformed into desired products in good to high yields, and this reaction can be easily scaled up to
Provided are compounds and compositions which modulate the level or activity of PIP4K2C. Also provided are methods for treating diseases or conditions by modulating (e.g., reducing) the level or activity of a PIP4K2C, comprising administering the compounds and compositions.