Anti-psma antibodies conjugated to nuclear receptor ligand polypeptides
A technology of antibodies and compounds, applied in the direction of anti-receptor/cell surface antigen/cell surface determinant immunoglobulin, peptide, specific peptide, etc., can solve the problem of limiting the usefulness of imaging agents
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example 1
[1347] Example 1: Synthesis of Compound 1
[1348] 1. Displayed in Figure 8 The detailed synthesis of compound 1 in
[1349] 1a. Synthesis of Compounds 1-3
[1350] Add dexamethasone 1-1 (0.4 g, 1.02 mmol) and N,N'-disuccinimidyl carbonate (0.4 g, 1.33 mmol) in DCM (4 ml) and THF (4 ml) at room temperature DIEA (0.36ml, 2.04mmol) was added to the mixture. The mixture was stirred overnight at room temperature. The mixture was concentrated and the crude product was purified by column chromatography. Obtained 0.13 g of 1-3 (24%) as a white solid. LCMS m / z=534[M+H]+
[1351] 1b. Synthesis of Compound 1-7
[1352] To a mixture of 1-4 (0.3g, 0.6mmol), 1-5 (0.12g, 0.66mmol) and EDC (0.2g, 1.2mmol) in DMF (6ml) was added 1N NaHCO3 (1.8mmol) at 0°C ) solution. The mixture was stirred overnight at room temperature. The mixture was extracted with EtOAc (3 x 30ml), and the mixture was washed with 0.5M HCl and brine. The organic layer was dried with anhydrous MgSO4. The organi...
example 2
[1359] Example 2: Synthesis of Compound 2
[1360] 2. Shown in Figure 9 The detailed synthesis of compound 2 in
[1361] 2a. Synthesis of Compound 2-2
[1362] To a mixture of 1-3 (0.1 g, 0.19 mmol) and tert-butyl 2-aminoethylcarbamate (30 g, 0.19 mmol) in acetonitrile (2 ml) was added DIEA (0.098 ml, 0.56 mmol) at room temperature. The mixture was stirred overnight at room temperature. The white precipitate was filtered and washed with diethyl ether to give the product 2-1 as a white solid.
[1363] A mixture of 2-1 (0.1 g) and 4N HCl in dioxane (1 ml) was stirred at room temperature for 1 hour. The mixture was concentrated under reduced pressure to give product 2-2 as a white solid. The product was used without further purification. LCMS m / z=479[M+H]+
[1364] 2b. Synthesis of Compound 2-4
[1365] To a mixture of 2-2 (0.09 g, 0.188 mmol) and Fmoc-Val-Cit-PAB-PNP (0.159 g, 0.21 mmol) in DMF (1 ml) was added DIEA (0.16 ml, 0.94 mmol) at room temperature. The mixture...
example 3
[1372] Example 3: Synthesis of Compound 3
[1373] 3. Shown in Figure 10 The detailed synthesis of compound 3 in.
[1374] 3a. Synthesis of Compound 3-1
[1375] To a solution of compound 3 (600 mg, 1.125 mmol) in 0.5 mL DMF was added tert-butyl methyl(2-(methylamino)ethyl)carbamate (127 mg, 0.675 mmol). The resulting solution was stirred at room temperature for 2 hours. The reaction mixture was diluted with EtOAc and washed with H2O, brine, dried over Na2SO4, then concentrated to dryness. The residue was purified by flash column chromatography to obtain 170 mg of compound 3-1. MS(ESI) m / z 607[M+H].
[1376] 3b. Synthesis of compound 3-2
[1377] Compound 3-1 (170 mg) was treated with 50% TFA in DCM. The reaction was concentrated to dry after 30 min. The product was used directly in the next step without further purification.
[1378] 3c. Synthesis of compound 3-3
[1379] Add Fmoc-Val-Cit-PAB-OPNP (215 mg, 0.28 mmol), HOBt (21.4 mg, 0.14 mmol) and DIEA (99 μl, 0.56...
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