3-甲胺基哌啶二盐酸盐的合成

3-Methylaminopiperidine dihydrochloride, a key intermediate for fluoroquinolone antibacterial balofloxacin, was synthesized from 3-aminopyridine by formylation, reduction and catalytic hydrogenation with an overall yield of 44%.

法西多曲的合成

胡椒醛与丙二酸二乙酯经缩合、催化氢化、水解、Mannich反应并脱羧得胡椒丙烯酸,与氯化亚砜反应得酰氯后,再经与L-丙氨酸苄酯对甲苯磺酸盐缩合,与硫代乙酸加成、异丙醇重结晶制得法西多曲,总收率约为21%。