A facile synthesis of the spiroindoline-based growth hormone secretagogue,MK-677  

作　　者：Xian Liang Qi Er Qun Yang Jun Tao Zhang Tao Wang Xiao Ping Cao 

机构地区：[1]State Key Laboratory of Applied Organic Chemistry and College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, China

出　　处：《Chinese Chemical Letters》2012年第6期661-664,共4页中国化学快报（英文版）

基　　金：supported by the National Basic Research Program of China(973 Program,No.2010CB833203);the National Natural Science Foundation of China(Nos.20972060 and 21061160494)

摘　　要：A facile and improved route for the synthesis of the orally active spiroindoline-based growth hormone secretagogue, MK-677 was described. The key step adopted the Fischer indole/reduction strategy. The preparation of the key intermediates N-protected piperidine carboxaldehyde 5 and the N-Boc-O-benzyl-D-serine （2） are also optimized.A facile and improved route for the synthesis of the orally active spiroindoline-based growth hormone secretagogue, MK-677 was described. The key step adopted the Fischer indole/reduction strategy. The preparation of the key intermediates N-protected piperidine carboxaldehyde 5 and the N-Boc-O-benzyl-D-serine （2） are also optimized.

关 键 词：MK-677 Synthesis Improved route Fischer indole/reduction 

分 类 号：X503.1[环境科学与工程—环境工程] TQ460.4[化学工程—制药化工]