4-(dihydroxyacetyl-L-serine)-goserelin as well as preparation method and application thereof
A technology of goserelin and preparation, applied in the field of medicine, can solve problems such as lack of research
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[0036] Example 1 Preparation of 4-(diglycolyl-L-serine)-goserelin
[0037] Step 1: Add 500 mg of goserelin, 50 mg of glycolide, and 5 ml of DMF solvent to a 10 ml vial, and react at room temperature for 24 hours.
[0038] Step 2: The reaction solution in step 1 was separated by preparative high performance liquid chromatography (chromatographic column: phenomenonex, luna 5 μm, 250×21.20mm, S / N: 443257-2, flow rate 20ml / min, detection wavelength 220nm), at 0.5 % Phosphoric acid aqueous solution-acetonitrile was used as the mobile phase, the ratio of acetonitrile was 20%-40% for gradient elution, the chromatographic peak was collected with a retention time of 14.03min, and a total of 750ml of eluent was collected.
[0039] Step 3: Mix the reversed-phase silica gel with methanol, stir, homogenize and pack the column, replace the methanol with purified water, add the eluent obtained in step 2 to the reversed-phase silica gel chromatography column with a peristaltic pump, adjust th...
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