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[reaction: see text] A zirconocene-mediated ring contraction of 4-vinylfuranosides generated either from d-arabinose or d-glucose is followed by sequential oxidation to the ketone and alkynyl Grignard addition. The resulting cis-cyclobutanediols are subjected in turn to thermal rearrangement and intramolecular oxymercuration-demercuration. The regiochemistry of the final ring closure is controlled by the nature of R. 相似文献
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Valentina Di Iorio Stefano Boschi Cristina Cuni Manuela Monti Stefano Severi Giovanni Paganelli Carla Masini 《Molecules (Basel, Switzerland)》2022,27(13)
Since prostate cancer is the most commonly diagnosed malignancy in men, the theranostic approach has become very attractive since the discovery of urea-based PSMA inhibitors. Different molecules have been synthesized starting from the Glu-urea-Lys scaffold as the pharmacophore and then optimizing the linker and the chelate to improve functional characteristics. This article aimed to highlight the quality aspects, which could have an impact on clinical practice, describing the development of an Investigational Medicinal Product Dossier (IMPD) for clinical trials with [177Lu]Lu-PSMA-I&T in prostate cancer and other solid tumors expressing PSMA. The results highlighted some important quality issues of the final preparation: radiolabeling of PSMA-I&T with lutetium-177 needs a considerably longer time compared with the radiolabeling of the well-known [177Lu]Lu-PSMA-617. When the final product was formulated in saline, the stability of [177Lu]Lu-PSMA-I&T was reduced by radiolysis, showing a decrease in radiochemical purity (<95% in 24 h). Different formulations of the final product with increasing concentrations of ascorbic acid have been tested to counteract radiolysis and extend stability. A solution of 20 mg/mL of ascorbic acid in saline prevents radiolysis and ensures stability over 30 h. 相似文献
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[reaction: see text] The ring contraction induced by treatment of 4-vinylfuranosides with zirconocene in the presence of boron trifluoride etherate can be rendered highly diastereoselective by proper adjustment of substituent stereochemistry. The two competing transition states that are seemingly involved appear to be usefully sensitive to nonbonded steric interactions. 相似文献
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Experimental Mechanics - Metaconcrete is a new concept of concrete, showing marked attenuation properties under impact and blast loading, where traditional aggregates are partially replaced by... 相似文献
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