1′-叔丁氧羰基-5-氟-螺-(吲哚啉-3,4′-哌啶)的合成

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

采用有效的方法合成了标题化合物。首先用三氟乙酸酐对1-N进行保护,然后用钯碳(Pd/C)还原1′-N的Cbz,并用Boc酸酐将1′-N加以保护得到1-三氟乙酰基-1′-叔丁氧羰基-5-氟-螺-(吲哚啉-3,4′-哌啶),最后,在碱性条件下,1-三氟乙酰基-1′-叔丁氧羰基-5-氟-螺-(吲哚啉-3,4′-哌啶)选择性的离去1-N保护基三氟乙酸酐得到标题化合物。

An efficient method was adopted to synthesize the title compound. Firstly, 1-N was protected by trifluoroacetic anhydride and then 1-trifluroacelyl-1′-Cbz-5-fluoro-spiro-（ indoline-3, 4′- piperidine） after being subjected to hydrogenolysis with 10% Pd supported on C in EtOH was protected by Boc anhydride in 1′-N to give 1-trifluroacelyl-1′-Boc-5-fluoro-spiro-（ indoline-3, 4′-piperidine）. Finally 1-N was selectively deprotected by trifluo- roacetic anhydride to yield title compound.