Organic Process Research and Development p. 1707 - 1717 (2020)
Update date:2022-07-30
Topics:
Chen, Yibo
Wu, Zenong
Yang, Zhezhou
Zhang, Fuli
Zhang, Tao
Zhao, Weili
An improved kilogram-scale process of synthesis of nalbuphine was developed by investigating the critical parameters. Ten process-related impurities were identified, of which the source and control strategy was elucidated. Moreover, tetramethylammonium triacetoxyborohydride (Me4NBH(OAc)3) was developed to reduce the imine and ketone in one pot. As a result, 6-β-epimer was significantly controlled to only 0.08% in the crude nalbuphine. The improved process was robust at kilogram scale in 60.4% overall yield with 99.95% high-performance liquid chromatography (HPLC) purity.
View MoreShandong Shouguang Songchuan Industrial Additives Co.,Ltd
Contact:+86-536-8566856
Address:Shouguang,Shandong,China
Contact:+86-518-81061113
Address:No. 8 Lingzhou Road, Lianyungang, Jiangsu, China
Qingdao Kylin Trading Co., Ltd.
Contact:0086-532-68979884/58972912/68972263/65/88171519
Address:Room 2308,A building International Trade Center No.230 Changjiang Middle Road of Qingdao Economic Development Zone,Shandong,China.
Contact:0512-63006287
Address:no.88.YISHENG Road,etdz-WUJIANG,SUZHOU,CHINA
Tianjin Tongde Biological Technology Co., Ltd.
Contact:86-22-23309138
Address:Room 402, bulidingE3 Detection certification park, XiQingDistrict, Tianjin City
Doi:10.1016/j.bmcl.2003.12.023
(2004)Doi:10.1055/s-2005-865296
(2005)Doi:10.1016/S0040-4020(01)88580-X
(1983)Doi:10.1021/je00035a030
(1984)Doi:10.1248/cpb.31.538
(1983)Doi:10.1021/ol051342i
(2005)