On June 25, 2020, Blanc, Jean-Baptiste; Khan, Nawaz; Kramer, Christian; Lerner, Christian; Pflieger, Philippe; Stoll, Theodor; Yang, Song published a patent.Electric Literature of 1251006-64-0 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 A is C2-9 heterocycloalkyl, C3-12 cycloalkyl, C6-14 aryl and C1-13 heteroaryl; R1 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R2 is H, OH, carboxyl, amino, etc.; R3, R4 and R5 are independently H and OH; R6 is H, halo, C1-6 alkyl, NO2, CN, etc.; R7 and R13 are independently H, halo and C1-6 alkyl; R8, R9, R10, R11 and R12 are independently H, halo, amino, C1-6 alkoxycarbonyl-C1-6 alkoxy, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 4-((3-(2,3-difluoro-4-methoxyphenyl)imidazo[1,2-a]pyrazin-8-yl)amino)-2-ethylbenzoic acid with tert-Bu cis-N-(3-aminocyclobutyl)carbamate; the resulting 4-((3-(2,3-difluoro-4-methoxyphenyl)imidazo[1,2-a]pyrazin-8-yl)amino)-2-ethylbenzoic acid underwent hydrolysis to give compound II. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.084μM. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Electric Literature of 1251006-64-0
The Article related to imidazopyrazine preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Electric Literature of 1251006-64-0
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem