Goserelin acetate solid-phase synthesis method

摘要: The invention relates to a goserelin acetate solid-phase synthesis method, which comprises the following steps: HBTU/DIPEA is employed as condensation system, Fmoc-Ser-OH, Fmoc-Trp-OH are successively coupled; whole-protection lysate with corresponding voluminal amount according 10 times of resin weight added, carrier 2-CTC Resin in an intermediate removed, all side chain protective groups reserved; adjusted slight alkaline by using DIPEA(N,N-diisopropylethylaine), semicarbazide hydrochloride and PyBop(1H-benzotriazole-1-oxygen tripyrrole alkyl hexafluorophosphate) (used for coupling agent peptide) added reaction coupling, peptide solution group obtained; 20% TFA/DCM freezing ether settling obtain white solid crude peptide; dried under vacuum solving methyl alcohol, ammonium formate Pa/c hydrogenation remove sequence. According invention, phenomena can be avoided, target purity increased, yield high, operation convenient feasible, tracked controlled, whole process benefit enlarged production.