| 摘要 |
The present invention relates to a process for the preparation of perhydroquinoxaline compounds according to the general formula (1) comprising the steps of a) reacting 5,6,7,8-tetrahydroquinoxalin-5-ol with a protection agent; b) catalytically hydrogenating the PG protected 5,6,7,8-tetrahydroquinoxalin-5-ol; c) chiral resolution of the racemic PG protected cis,cis-decahydroquinoxalin-5-ol; d) reacting the PG protected (4aS,5R,8a S)-decahydroquinoxalin-5-ol with a reagent X2-R1; e) deprotecting the PG protected hydroxy group; f) reacting the α,β-aminoalcohol with sulfuryl chloride; g) reacting the 1,2,3-oxathiazolidine 2,2-dioxide with an amine HNR2R3; h) reacting the cis,trans-5-amino-decahydroquinoxaline with an activated carboxylic acid derivative ZCH2COY to provide for the compound of formula (1); i) optionally converting the compound of formula (1) to pharmaceutically acceptable salts by reaction with the corresponding acid. Further, the invention relates to PG protected cis,cis- decahydroquinoxalin-5-ol, PG-protected (4a S,5R,8a S)-decahydroquinoxalin-5-ol and PG protected (4a R,5S,8a R)-decahydroquinoxalin-5-ol, and its preparation in enantiomeric pure forms. |
