1,2-Dichloroethane → 3-(5-5,6,7,8-Tetrahydro-[1,8]naphthyridin-2-yl-pentanoylamino)-propionic acid

A mixture of acid 1-6 (10.8 mg, 0.04 mmol), EDC (7.7 mg, 0.04 mmol), HOBT (5.4 mg, 0.04 mmol) and NMM (0.026 mL, 0.24 mmol) in DMF (1 mL) was agitated until clear solution. After 30 minutes, amine 12-1 was added. The solution was agitated for one minute and then let stand for 18 h. The solution was diluted with ethyl acetate, washed with sat. NaHCO3 and H2O. Following evaporative removal of the solvent, the residue was dissolved in 90:10 TFA/H2O (1 ml). After 2 h, the solvents were evaporated to give acid 12-2.

1. stirringThe solution was agitated for one minute
2. waitlet stand for 18 h
3. washwashed with sat. NaHCO3 and H2O
4. customremoval of the solvent
5. dissolutionthe residue was dissolved in 90:10 TFA/H2O (1 ml)
6. waitAfter 2 h
7. customthe solvents were evaporated

ORD-Eintrag

ord-935506d683a04ad3b3221a270e67b742

Quelldatensatz

uspto-grants-2000_04

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US06048861