| 摘要 |
<p>PURPOSE:To obtain the desired isomer of the titled compound which is an intermediate for medicines, etc. in high yield, by reacting a desired isomer of a specific compound derived from serine or cysteine with 2-aminobenzenethiol, and subjecting the resultant product to the ring closure reaction, etc. CONSTITUTION:A compound expressed by formula I (X is halogen; R1 is alkanoyl, benzyloxy, carbonyl or usual protecting group of the amino group; R2 is hydroxyl group or loer alkoxyl), and derivable from serine or cysteine is reacted with 2-aminobenzenethiol in a suitable solvent in the presence of a deacidifying agent, preferably sodium hydroxide, within 0 deg.C-the boiling point temperature range to afford a compound expressed by formula II, which is then subjected to the ring closure reaction or further the group R1 is eliminated to afford the aimed compound expressed by formula III. The ring closure reaction is carried out using a dehydrating agent, e.g. dicyclohexycarbodiimide, etc.</p> |
