1,1'-Carbonyldiimidazole → HCID 68646904, compound

Participants

Reaction Conditions

Reaction Steps

106.3 5-Chloro-thiophene-2-carboxylic acid (0.94 g) was dissolved in THF (10 ml) and CDI (0.94 g) was added. This mixture was stirred at 25° C. for 30 min. A solution of (3-amino-pyrrolidin-1-yl)-oxo-acetic acid ethyl ester trifluoroacetate (1.57 g), dissolved in THF (10 ml) and DIEA (0.89 ml), is added to the reaction mixture. The obtained reaction mixture was stirred for 18 h at 25° C. Finally, the reaction mixture was evaporated to dryness. The crude product was purified by chromatography (silica gel; gradient: CH2Cl2 to CH2Cl2/MeOH 98:2) to give {3-[(5-chloro-thiophene-2-carbonyl)-amino]-pyrrolidin-1-yl}-oxo-acetic acid ethyl ester (1.9 g) as an orange oil. MS 331.3 ([M+H]+, Cl-isotopes).

Provenance & Evidence