反应详情

Add methanol (1 mL) and triethylamine (0.36 mL; 1.0 equiv; 2.58 mmoles) to a vial containing methyl 6-imino-6-methoxy-hexanoate (0.542 g; 1.00 equiv; 2.58 mmoles), followed by a solution of formylhydrazine (0.155 g 1.0 equiv; 2.58 mmoles) in methanol (3 mL). Stir at room temperature for 18 hours, then heat to 70° C. for 3 hours. Concentrate the mixture, then dilute with ethyl acetate (30 mL) and filter. Concentrate the filtrate to afford methyl 5-(4H-1,2,4-triazol-3-yl)pentanoate (0.498 g; 105%) as a colorless oil: MS (m/z): 184 (M+1).

1. temperatureheat to 70° C. for 3 hours
2. concentrationConcentrate the mixture
3. additiondilute with ethyl acetate (30 mL)
4. filtrationfilter
5. concentrationConcentrate the filtrate