In this paper,brinzolamide(S)-isomer was synthesized from 3-(2-bromoacetyl)-5-chloro-2-thiophenesulfonamide over five-step reactions of reduction cyclization,N-alkylation,sulfamation,amino protecting and amination fir...In this paper,brinzolamide(S)-isomer was synthesized from 3-(2-bromoacetyl)-5-chloro-2-thiophenesulfonamide over five-step reactions of reduction cyclization,N-alkylation,sulfamation,amino protecting and amination firstly,in total yield of 23%.The structures were characterized by 1H NMR、MS.The mixture of brinzolamide and its(S)-isomer was analyzed by HPLC indicating the resolution factor was 3.022 between brinzolamide and its(S)-isomer through column selection and factor modulation.The e.e.value of synthesized brinzolamide(S)-isomer was 96.9%.展开更多
文摘In this paper,brinzolamide(S)-isomer was synthesized from 3-(2-bromoacetyl)-5-chloro-2-thiophenesulfonamide over five-step reactions of reduction cyclization,N-alkylation,sulfamation,amino protecting and amination firstly,in total yield of 23%.The structures were characterized by 1H NMR、MS.The mixture of brinzolamide and its(S)-isomer was analyzed by HPLC indicating the resolution factor was 3.022 between brinzolamide and its(S)-isomer through column selection and factor modulation.The e.e.value of synthesized brinzolamide(S)-isomer was 96.9%.
