Chiral synthesis of n-{ 3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl} -1-[2,3-dihydroxy-propyl]cyclopropanesulfonamides

摘要

The disclosure relates to an method of preparing (S)- and (R)-enantiomers of N-{ 3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl} -1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide ((S)-14 and (R)-14) and to the intermediate compounds used in this method. The intermediate compounds include: 1-{ [(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl} cyclopropanesulfonyl bromide Butyl 1-{ [(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl} cyclopropanesulfonate Butyl 1-[(2S)-2,3-dihydroxypropyl]cyclopropanesulfonate Butyl 1-[(2S)-3-chloro-2-hydroxypropyl]cyclopropanesulfonate Butyl 1-[(2R)-2-hydroxy-3-(tetrahydro-2H-pyran-2-yloxy)propyl]cyclopropane sulfonate.