Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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An Effective Acylation of Cephalosporins Using 1-Methanesulfonyloxy-6-trifluoromethylbenzotriazole$^\dag$

  • Lee, Cheol-Hae (Division of Organic Chemistry, Korea Research Institute of Chemical Technology) ;
  • Moon, Chi-Jang (Division of Organic Chemistry, Korea Research Institute of Chemical Technology) ;
  • Kim, Kyeong-Sook (Division of Organic Chemistry, Korea Research Institute of Chemical Technology) ;
  • Kim, Jae-Hak (Division of Organic Chemistry, Korea Research Institute of Chemical Technology) ;
  • Kim, Dae-Whang (Division of Organic Chemistry, Korea Research Institute of Chemical Technology)
  • Published : 1987.08.20
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Abstract

A new coupling agent, 1-methanesulfonyloxy-6-trifluoromethyl-benzotriazole (3), was prepared by the reaction of 1-hydroxy-6-trifluoromethylbenzotriazole (1) and methanesulfonyl chloride. 3 was reacted with 2-(2-amino-4-thiazolyl)-2-synalkoxyi minoacetic acid (4) to give a mixture of active intermediates (5 and 6), which was treated with 7-aminocephalosporanic acid derivatives (10) to afford cephalosporin derivatives (11) in short reaction time with high yields.

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References

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Cited by

  1. Synthese von 3-α-Chlorvinylcephalosporinen vol.324, pp.2, 1991, https://doi.org/10.1002/ardp.19913240213
  2. Synthesis and Pharmacokinetic Profile of 3-Methoxymethyl Cephalosporin Prodrugs vol.21, pp.5, 1998, https://doi.org/10.1007/bf02975375