On June 25, 2020, Cheng, Zhanling; Khan, Nawaz; Kramer, Christian; Lerner, Christian; Nettekoven, Matthias; Pflieger, Philippe; Puellmann, Bernd; Schmitt, Sebastien; Stoll, Theodor; Wang, Jianhua; Yang, Song published a patent.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Novel imidazopyrazine derivatives as antibacterials and their preparation. And the patent contained the following:
The invention provides imidazopyrazine derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and related diseases. Compounds of formula I wherein R1 is R12-C1-6 alkyl-X-C1-6 alkyl; R2 is H, C1-6 alkyl, C1-6 haloalkyl, C1-6 cyanoalkyl, etc.; R3 is H, halo, C1-6 alkyl, NO2, CN, etc.; R4 and R10 are independently H, halo and C1-6 alkyl; R5, R6, R7, R8 and R9 are independently H, halo, amino, C1-6 alkoxycarbonyl-C1-6 alkoxy, etc.; R11 is H, halo and C1-6 alkyl; R12 is H, vinyl, C2-6 alkynyl, OH, etc.; X is O, NH, S, SO, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II•TFA was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.12μM. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate
The Article related to imidazopyrazine preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Safety of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem