	US 11,717,575 B2
	One-pot process for preparing intermediate of antibody-drug conjugate
Zhaoxing Yu, Shandong (CN); Xinfang Li, Shandong (CN); Mingchao Lan, Shandong (CN); and Xinjie Mao, Shandong (CN)
Assigned to MABPLEX INTERNATIONAL CO., LTD., Shandong (CN)
Appl. No. 15/733,309
Filed by MABPLEX INTERNATIONAL CO., LTD., Shandong (CN)
PCT Filed Feb. 13, 2020, PCT No. PCT/CN2020/074987 § 371(c)(1), (2) Date Jun. 23, 2020, PCT Pub. No. WO2020/233174, PCT Pub. Date Nov. 26, 2020.
Claims priority of application No. 201910420868.X (CN), filed on May 20, 2019; application No. 201910916198.0 (CN), filed on Sep. 26, 2019; application No. 201910916200.4 (CN), filed on Sep. 26, 2019; application No. 201910916242.8 (CN), filed on Sep. 26, 2019; application No. 201910916470.5 (CN), filed on Sep. 26, 2019; application No. 201910916508.9 (CN), filed on Sep. 26, 2019; and application No. 201910916510.6 (CN), filed on Sep. 26, 2019.
Prior Publication US 2021/0085799 A1, Mar. 25, 2021
Int. Cl. A61K 47/68 (2017.01); A61K 47/65 (2017.01); A61K 45/06 (2006.01)

CPC A61K 47/6801 (2017.08) [A61K 47/65 (2017.08); A61K 45/06 (2013.01)]

5 Claims

1. A process for preparing an intermediate of antibody-drug conjugate comprising a linker portion and a drug portion, wherein the intermediate of antibody-drug conjugate is Py-MAA-Val-Cit-PAB-D or MC-Val-Cit-PAB-D, wherein Py-MAA-Val-Cit-PAB or MC-Val-Cit-PAB in the intermediate is the linker portion, and D in the intermediate represents linked drug portion comprising free amino groups, wherein the process comprises the following reaction route:

wherein the preparation process is a one-pot process in which two steps are carried out in one system, wherein, the organic base 1 and the organic base 2 are each independently one or two of N,N-diisopropylethylamine and pyridine, and wherein the triazole catalyst is one or more of 1-hydroxybenzotriazole, 1-hydroxy-7-azobenzotriazole, 1-hydroxy-1H-1,2,3-triazole-4-carboxylic acid ethyl ester.