On September 24, 2021, Zhao, Zhiming; Liu, Lifeng; Liu, Qingyun; Wang, Hailong; Guan, Huiping; Da, Chenxiao; Chen, Xi; Xu, Guiliang published a patent.Safety of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate The title of the patent was Polyheterocyclic substituted pyrimidine or pyridylamine derivatives, compositions thereof and medical applications thereof. And the patent contained the following:
The invention discloses the polyheterocyclic substituted pyrimidine or pyridylamine derivatives (e.g., I) as adenosine receptor antagonists, which have significant adenosine A2A receptor and/or adenosine A2B receptor antagonistic activities. For example, 3-(2-amino-6-(1-((5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-2-yl)methyl)-1H-1,2,3-triazol-4-yl)pyrimidin-4-yl)-2-methylbenzonitrile (I) was prepared via reaction of 3-bromo-2-methylbenzonitrile with bis(pinacolato)diboron, followed by Suzuki coupling reaction with 2-amino-4,6-dichloropyrimidine, followed by Sonogashira coupling with (triisopropylsilyl)acetylene, followed by Click reaction with 2-(azidomethyl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole. The title compounds can be used in medicines for treating diseases mediated by adenosine A2A receptor and/or adenosine A2B receptor. The experimental process involved the reaction of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate(cas: 153597-59-2).Safety of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate
The Article related to pyrimidine pyridylamine triazole adenosine receptor antagonist immunomodulator antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics