CAS: 112257-20-2; 1-Cbz-3-Aminoazetidine

相似化合物

959957-92-7 112257-42-8 102065-89-4

上下游产品

benzyl 3-[(tert-butoxycarbonyl)amino]azetidine-1-carboxylate

📜Benzyl 3-[(Tert-Butoxycarbonyl)Amino]Azetidine-1-Carboxylate置于三氟乙酸体系中,用 二氯甲烷 用作溶剂,化学反应 3.0H,反应生成1-叔丁氧羰基-3-胺基环丁胺
参考文献:Challenges In The Development Of An M 4 Pam Preclinical Candidate: The Discovery,Sar,And In Vivo Characterization Of A Series Of 3-Aminoazetidine-Derived Amides
标题:Challenges In The Development Of An M 4 Pam Preclinical Candidate: The Discovery,Sar,And In Vivo Characterization Of A Series Of 3-Aminoazetidine-Derived Amides
摘要:This Letter Details The Continued Chemical Optimization Of A Novel Series Of M4 Positive Allosteric Modulators (Pams) Based On A 5-Amino-Thieno[2,3-C] Pyridazine Core By Incorporating A 3-Amino Azetidine Amide Moiety. The Analogs Described Within This Work Represent The Most Potent M4 Pams Reported For This Series To Date. The Sar To Address Potency,Clearance,Subtype Selectivity,Cns Exposure,And Pgp Efflux Are Described. This Work Culminated In The Discovery Of Vu6000918,Which Demonstrated Robust Efficacy In A Rat Amphetamine-Induced Hyperlocomotion Reversal Model At A Minimum Efficacious Dose Of 0.3 Mg/kg. (C) 2017 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2017.05.014