| 摘要 |
[PROBLEMS] To provide a process for industrially producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-ethyl]-1,3-propanediol hydrochloride (compound (I)), which is a compound having excellent immunosuppressive activity. [MEANS FOR SOLVING PROBLEMS] The process, which is for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-ethyl]-1,3-propanediol hydrochloride, is characterized by reacting 4-(3-benzyloxyphenylthio)-2-chlorobenzaldehyde with ethyl diethylphosphonoacetate in a solvent in the presence of a base to obtain ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate, reducing the ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate, subjecting the reduced compound to mesylation, iodination, and nitration to yield 1-benzyloxy-3-[3-chloro-4-(3-nitropropyl)phenylthio]benzene, converting it to 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol with formaldehyde, and then reducing it.
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