With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.137076-54-1,2-(4,7,10-Tris(2-(tert-butoxy)-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetic acid,as a common compound, the synthetic route is as follows.
To a DOTA-tra-tBu ester (28.6 mg, 0.05 mmol) in 2 mL DMF, DIPEA (24.8 mg, 0.192 mmol), HOBt (16.2 mg, 0.096 mmol), 43 (50 mg, 0.048 mmol) and EDCI (18.2 mg, 0.096 mmol) were added at 0 C. The mixture was stirred at room temperature for overnight, then 15 mL EtOAc was added to above solution. It was then washed with H20 (5 mL x 2) and brine (5 mL), dried over MgS04, and filtered. The filtrate was concentrated, and the residue was purified by FC (DCM/MeOH/NH4OH = 95/5/0.5) to give 43 as a colorless oil (yield: 26 mg, 35.6%): HRMS calcd. for C39H64N5Oio (1/2M + H)+: 762.4653, found 762.4787., 137076-54-1
137076-54-1 2-(4,7,10-Tris(2-(tert-butoxy)-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl)acetic acid 11606627, acatalyst-ligand compound, is more and more widely used in various fields.
Reference£º
Patent; FIVE ELEVEN PHARMA INC.; KUNG, Hank F.; PLOESSL, Karl; CHOI, Seok Rye; ZHA, Zhihao; WU, Zehui; (131 pag.)WO2017/116994; (2017); A1;,
Metal catalyst and ligand design
Ligand Template Strategies for Catalyst Encapsulation – NCBI