1-叔丁氧羰基-5-氟-螺-(吲哚啉-3,4′-哌啶)盐酸盐的合成

Synthesis of 1-Boc-5-fluoro-spiro-(indoline-3,4'-piperidine) hydrochloride

采用了方便的方法由1-氢-1′-苄氧羰基-5-氟-螺-(吲哚啉-3,4′-哌啶)合成了标题化合物。首先用Maligres等报道的典型方法合成了1-氢-1′-苄氧羰基-5-氟-螺-(吲哚啉-3,4′-哌啶),再使用二碳酸叔丁酯对1-N进行保护,然后用10%钯碳(Pd/C)氢解1′-N的Cbz,最后,室温下得到重要药物中间体盐酸盐。

A convenient method for synthesis of 1-Boc-5-fluorospiro- （ indoline-3,4＇-piperidine ） hydrochloride hydroehloride was developed. The compound 1-H-1＇-Cb2-5-fluoro-spiro-（indoline- 3,4＇-piperidine） was prepared by using the typical synthetic approach reported by Maligres et al. Cbz in 1＇-N was hydrogenated in the presence of 10% palladium supported on charcoal resulting in the compound 1-Boc-1＇-H-5-fluoro-spiro-（indoline-3, 4＇- piperidine） after 1-N of 1-H-1＇-Cb2-5-fluoro-spiro-（ indoline- 3,4＇- piperidine） was protected by Boc anhydride. Finally, the key medicine intermediate 1-Boc-5-fluoro-spiro-（ indoline-3, 4＇- piperidine） hydrochloride hydrochloride at room temperature was obtained.