US 12,325,712 B2
Method for preparing naldemedine
Hyunik Shin, Suwon-si (KR); and Hyoseon Lee, Bucheon-si (KR)
Assigned to YONSUNG FINE CHEMICAL CO., LTD., Hwaseong-si (KR)
Appl. No. 17/604,605
Filed by YONSUNG FINE CHEMICAL CO., LTD., Hwaseong-si (KR)
PCT Filed Apr. 14, 2020, PCT No. PCT/KR2020/005007
§ 371(c)(1), (2) Date Oct. 18, 2021,
PCT Pub. No. WO2020/213911, PCT Pub. Date Oct. 22, 2020.
Claims priority of application No. 10-2019-0046088 (KR), filed on Apr. 19, 2019.
Prior Publication US 2022/0194953 A1, Jun. 23, 2022
Int. Cl. C07D 489/08 (2006.01)
CPC C07D 489/08 (2013.01) 14 Claims
 
1. A process for preparing naldemedine of the following formula (1), which comprises the steps of:
(i) reacting a compound of the following formula (2) with diethyl pyrocarbonate, followed by treating with a base to obtain a compound of the following formula (3);
(ii) subjecting the compound of the following formula (3) to a combination reaction with a compound of the following formula (4), followed by adding hydrochloric acid to obtain a compound of the following formula (5); and
(iii) deprotecting the compound of the following formula (5):

OG Complex Work Unit Chemistry