The microwave-assisted intramolecular [3 + 2] cycloaddition reaction of azomethine ylides to activated and nonactivated alkenes and alkynes is described. The procedure allows the synthesis of pyrrolidines and pyrrole products in good to excellent overall yields in short reaction times. It appears from parallel comparative studies that the microwave procedure favors the reaction times and overall purity of the crude reaction mixture. The reactions can also be performed in the absence of solvent. [reaction: see text]
Metabolic glycoengineering with unnatural sugars became a valuable tool for introducing recognition markers on the cell membranes via bioorthogonal chemistry. By using this strategy, we functionalized the surface of tumor...
Microwave-Assisted [3 + 2] Cycloadditions of Azomethine Ylides. -The influence of microwaves on the cycloaddition reaction of O-allylic and O-propargylic salicylaldehydes with α-amino esters is studied and compared to simple heating. In all cases, the fused pyrrole derivatives are formed under microwave irradiation in significantly shorter reaction times. -(BASHIRHIARDES*, G.; SAFIR, I.; MOHAMED, A. S.; BARBOT, F.; LADURANTY, J.; Org. Lett. 5 (2003) 25, 4915-4918; Dep. Chim., Methodol. Synth. Biomol., Univ. Poitiers, F-86022 Poitiers, Fr.; Eng.) -Klein 16-129
Enhancing the selectivity of anticancer drugs currently used in the clinic is of great interest in order to propose patients more efficient chemotherapies with less side effects. In this context, we developed a -cyclodextrin trimer that binds to circulating albumin to form the corresponding bioconjugate in the bloodstream. This later can then entrap doxorubicin following its i.v. administration via the formation of a host-guest inclusion complex and deliver the drug in tumors. In this study, we demonstrate that the -cyclodextrin trimer improves the therapeutic efficacy of doxorubicin for the treatment of a subcutaneous murine Lewis lung carcinoma (LLC)
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