Preparation
1. In a three-necked flask, tetrahydrofuran and aspartic acid were mixed, and phosphorus oxychloride was added dropwise at low temperature. After reacting for 6 hours, the mixture was filtered to obtain a solid intermediate. 2. The solid intermediate was washed with anhydrous diethyl ether, dried, and then reacted with allyl alcohol, controlling the temperature and time. After the reaction, the pH was adjusted to 7 with triethylamine to precipitate the solid. 3. The solid was washed with diethyl ether and dried to obtain intermediate L-Asp-0A11. 4. L-Asp-0A11 was dissolved in sodium bicarbonate solution, and acetone and Fmoc-0Su were added. The pH was controlled at around 9, and the reaction was carried out at low temperature for 3 hours. 5. After the reaction, the product was washed with anhydrous diethyl ether, extracted with ethyl acetate, and concentrated to dryness after acidification, washing, and drying. 6. Finally, the target product, FMOC-ASP(OALL)-OH, was obtained by crystallization with petroleum ether.
Uses
Fmoc-Asp(OAll)-OH, is an amino acid building block used in peptide synthesis. With a growing peptide drug market the fast, reliable synthesis of peptides is of great importance.
