| abstract |
The invention provides a method for synthesizing deslorelin in a full liquid phase, which comprises the following steps: r is to be 4 ‑Pyr‑His(R 3 ) -Trp (Boc) -Ser (tBu) -Tyr (tBu) -D-Trp-Leu-OH and H-Arg (pbf) -Pro-NHEt are subjected to condensation reaction to obtain R 4 ‑Pyr‑His(R 3 ) -Trp (Boc) -Ser (tBu) -Tyr (tBu) -D-Trp-Leu-Arg (pbf) -Pro-NHEt, and then reacting in a cutting fluid to obtain deslorelin. Compared with the prior art, the invention has the advantages that the production process is green and mild by a full liquid phase synthesis method, no toxic reagent which is extremely toxic and easy to prepare is used, the purity of the produced product is high, the crude product can reach more than 90 percent, the cost is greatly reduced, and the method is very suitable for large-scale production. |