Chemoenzymatic synthesis of (S)-duloxetine using carbonyl reductase from Rhodosporidium toruloides
详细信息 查看全文
- 作者：Xiang Chen ; Zhi-Qiang Liu ; Chao-Ping Lin ; Yu-Guo Zheng ; zhengyg@zjut.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：Chemoenzymatic ; Duloxetine ; Carbonyl reductases ; Asymmetric synthesis ; (S)-3-(dimethylamino)-1-(2-thienyl)-1-propanol
- 刊名：Bioorganic Chemistry
- 出版年：2016
- 出版时间：April 2016
- 年：2016
- 卷：65
- 期：Complete
- 页码：82-89
- 全文大小：907 K
文摘
- •
An effective chemoenzymatic strategy was developed for (S)-duloxetine production.
- •
Carbonyl reductase from Rhodosporidium toruloides was employed in the key step.
- •
Cofactor regeneration was accomplished using RtSCR9 coupled glucose dehydrogenase.
- •
Production of chiral intermediate (S)-3a with so far the highest substrate loading.
- •
(S)-duloxetine was prepared in 60.2% yield from 2-acethylthiophene with >98.5% ee.