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1-(2-Aminoethylsulfonyl)-2-phosphorylpyrrolidines have been synthesized via boron trifluoride-catalyzed Arbuzov reaction of 2-ethoxy-1-(vinylsulfonyl)pyrrolidine with triethyl phosphite followed by aza-Michael reaction of thus obtained 2-phosphoryl-1-(vinylsulfonyl)pyrrolidine with secondary amines. The cytotoxicity of the prepared… Click to show full abstract
1-(2-Aminoethylsulfonyl)-2-phosphorylpyrrolidines have been synthesized via boron trifluoride-catalyzed Arbuzov reaction of 2-ethoxy-1-(vinylsulfonyl)pyrrolidine with triethyl phosphite followed by aza-Michael reaction of thus obtained 2-phosphoryl-1-(vinylsulfonyl)pyrrolidine with secondary amines. The cytotoxicity of the prepared 1-(2-aminoethylsulfonyl)-2-phosphorylpyrrolidines against M-Hela tumor cell line is comparable with that of tamoxifen, whereas the cytotoxicity against normal cell line is twofold lower.
Journal Title: Mendeleev Communications
Year Published: 2019
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