[CH3:1][O:2][C:3](=[O:16])[CH2:4][NH:5][C:6](=[O:15])[CH:7]=[CH:8][C:9]1[CH:14]=[CH:13][CH:12]=[CH:11][CH:10]=1.Cl.COC(=O)CN.CN1CCOCC1.[F:31]C1C=CC(C=CC(O)=O)=CC=1.C1(N=C=NC2CCCCC2)CCCCC1.ON1C2C=CC=CC=2N=N1>O1CCCC1>[CH3:1][O:2][C:3](=[O:16])[CH2:4][NH:5][C:6](=[O:15])[CH:7]=[CH:8][C:9]1[CH:10]=[CH:11][C:12]([F:31])=[CH:13][CH:14]=1
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.
読み込み中…
