In 2013,Zhang, Lei; Villalobos, Anabella; Beck, Elizabeth M.; Bocan, Thomas; Chappie, Thomas A.; Chen, Laigao; Grimwood, Sarah; Heck, Steven D.; Helal, Christopher J.; Hou, Xinjun; Humphrey, John M.; Lu, Jiemin; Skaddan, Marc B.; McCarthy, Timothy J.; Verhoest, Patrick R.; Wager, Travis T.; Zasadny, Kenneth published 《Design and Selection Parameters to Accelerate the Discovery of Novel Central Nervous System Positron Emission Tomography (PET) Ligands and Their Application in the Development of a Novel Phosphodiesterase 2A PET Ligand》.Journal of Medicinal Chemistry published the findings.Synthetic Route of C3H8ClNO The information in the text is summarized as follows:
To accelerate the discovery of novel small mol. central nervous system (CNS) positron emission tomog. (PET) ligands, we aimed to define a property space that would facilitate ligand design and prioritization, thereby providing a higher probability of success for novel PET ligand development. Toward this end, we built a database consisting of 62 PET ligands that have successfully reached the clinic and 15 radioligands that failed in late-stage development as neg. controls. A systematic anal. of these ligands identified a set of preferred parameters for physicochem. properties, brain permeability, and nonspecific binding (NSB). These preferred parameters have subsequently been applied to several programs and have led to the successful development of novel PET ligands with reduced resources and timelines. This strategy is illustrated here by the discovery of the novel phosphodiesterase 2A (PDE2A) PET ligand 4-(3-[18F]fluoroazetidin-1-yl)-7-methyl-5-{1-methyl-5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl}imidazo[5,1-f][1,2,4]triazine, [18F]PF-05270430 (5). In addition to this study using Azetidin-3-ol hydrochloride, there are many other studies that have used Azetidin-3-ol hydrochloride(cas: 18621-18-6Synthetic Route of C3H8ClNO) was used in this study.
Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Synthetic Route of C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.
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