Реакция #2275729

Уравнение реакции

3-Amino-azetidine-1-carboxylic acid tert-butyl ester

(3-trifluoromethyl-benzoylamino)-acetic acid

EDCI

HOBT

→

title compound

3-[2-(3-Trifluoromethyl-benzoylamino)-acetylamino]azetidine-1-carboxylic acid tert-butyl ester

Растворители

DCM

Условия реакции

Обработка

1. 1
   ДругоеThe reaction solution was partitioned between DCM and water
2. 2
   ПромывкаThe organic layer was washed with brine
3. 3
   Сушкаdried over anhydrous Na2SO4
4. 4
   Фильтрацияfiltered
5. 5
   Концентрированиеconcentrated
6. 6
   Другоеto give a yellow oil
7. 7
   Другоеpurified by silica gel column on a CombiFlash® system

Методика

3-Amino-azetidine-1-carboxylic acid tert-butyl ester (AstaTech, 1.2 g, 6.97 mmol) and (3-trifluoromethyl-benzoylamino)-acetic acid (Bionet Building Blocks, 1.57 g, 6.36 mmol) were treated with EDCI (Aldrich, 1.57 g, 6.36 mmol), HOBT (Aldrich, 1.22 g, 6.36 mmol) in DCM (10 mL) at room temperature for 4 hours. The reaction solution was partitioned between DCM and water. The organic layer was washed with brine, dried over anhydrous Na2SO4, filtered and concentrated to give a yellow oil, and purified by silica gel column on a CombiFlash® system using hexanes and ethyl acetate (from 10% ethyl acetate to 100% ethyl acetate) to afford the title compound as a white solid.

Источник