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With triethylamine; In acetonitrile; at 40℃;Inert atmosphere;
(1) preparative example of (2S,4S)-2-[(4-aminosulfonylphen-1-yl)iminomethylformyl]-4-thiol-1-(p-nitrobenzyloxycarbonyl)pyrrolidine (intermediate 1) 5-N-(4-nitrobenzyloxycarbonyl)-2-thia-5-azabicyclo[2.2.1]hept-3 -one (raw material 1) (1600 g, 5.19 mol) and <strong>[13009-99-9]mafenide acetate</strong> (raw material 2) (1219.2 g, 4.95 mol) were dissolved in acetonitrile, and the solution was warmed to 40 C. Triethylamine was added dropwise under nitrogen protection, and the reaction mixture was stirred to precipitate, filtered to obtain intermediate 1.
With triethylamine; In acetonitrile; at 40℃;Inert atmosphere; Large scale;
Intermediate 1 is (2S,4S)-2-[(4-aminosulfonylphen-1-yl)iminomethylformyl]-4-thiol-1-(p-nit robenzyloxycarbonyl)pyrrolidine. 5-N-(4-nitrobenzyloxycarbonyl)-2-thia-5-azabicyclo[2.2.1]hept-3-one (raw material 1) (1600 g, 5.19 mol) and <strong>[13009-99-9]mafenide acetate</strong> (raw material 2) (1219.2 g, 4.95 mol) were dissolved in acetonitrile, and the solution was warmed to 40 C. Triethylamine was added dropwise under nitrogen protection, and the reaction mixture was stirred to precipitate, filtered to obtain intermediate 1.
(4R,5S,6S)-3-[[(3S,5S)-N-(4-nitrobenzyloxycarbonyl)-5-[(4-aminosulfonylphen-1-yl)methyl]carbamoyl]-3-pyrrolidinyl]thio-6-[(R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid(4-nitrobenzyl) methyl ester[ No CAS ]
[(4R,5S,6S)-3-[(3S,5S)-5-[(4-aminosulfonylphen-1-yl)methyl]carbamoyl]-3-pyrrolidinyl]thio-6-[(R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo [3.2.0]hept-2-ene-2-carboxylic acid[ No CAS ]