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1. (WO2018120923) METHOD FOR PREPARING 1,4,7,10-TETRAAZACYCLODODECANE-1,4,7,10-TETRAACETIC ACID

Pub. No.:    WO/2018/120923    International Application No.:    PCT/CN2017/102056
Publication Date: Fri Jul 06 01:59:59 CEST 2018 International Filing Date: Tue Sep 19 01:59:59 CEST 2017
IPC: C07D 257/02
Applicants: VIWIT PHARMACEUTICAL CO., LTD.
山东威智医药工业有限公司
Inventors: MENG, Zhoujun
孟周均
HE, Yigang
何一刚
WEI, Yanjun
魏彦君
XING, Yanping
邢艳平
Title: METHOD FOR PREPARING 1,4,7,10-TETRAAZACYCLODODECANE-1,4,7,10-TETRAACETIC ACID
Abstract:
Disclosed is a method for preparing 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) of formula (II), comprising the following steps: carrying out an alkylation reaction on cyclen in formula (I) and XCH2COOR in the presence of an acid-binding agent in water; adjusting a pH value to separate out a crude product of DOTA; and recrystallizing. The preparation method of the present invention is applicable to large-scale industrial production of DOTA, the whole process does not need to adopt an ion-exchange resin or low-temperature refrigeration mode for purification, and the purity and yield of the product are higher.