4-Methylmorpholine → 4-Fluorocinnamoyl-glycine methyl ester

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

Following the general procedure described in example 1, step 2, for cinnamoyl-glycine methyl ester, glycine methyl ester hydrochloride (7.5 g) was suspended in tetrahydrofuran, cooled to 0° C., treated with N-methylmorpholine (8.4 ml, 1 equivalent), followed immediately by a precooled solution of 4-fluorocinnamic acid (10.0 g) in tetrahydrofuran, which had been pre-activated by treatment with dicyclohexylcarbodiimide (12.4 g, 1 equivalent) and 1-hydroxybenzotriazole (9.2 g). After work-up, 4-fluorocinnamoyl-glycine methyl ester was obtained as a white solid which was used for the next step without further purification.

Herkunft & Nachweise