반응 #2275729

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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

용매

DCM

반응 조건

후처리

1. 1
   기타The reaction solution was partitioned between DCM and water
2. 2
   세척The organic layer was washed with brine
3. 3
   건조dried over anhydrous Na2SO4
4. 4
   여과filtered
5. 5
   농축concentrated
6. 6
   기타to give a yellow oil
7. 7
   기타purified by silica gel column on a CombiFlash® system

실험 절차

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.

출처