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- W2228493699 abstract "1740 Objectives To simplify residual solvent analysis and speed up [11C]production, we demonstrate the fully automated loop syntheses of 11C-Raclopride, 11C-DASB, and 11C-PBR28 using ethanol as the only organic solvent for machine cleaning, 11C-methylation, HPLC purification and reformulation. Methods A GE Tracerlab FX C Pro has been modified as previously reported for loop chemistry. The corresponding precursor is dissolved into 100 uL of absolute ethanol and loaded onto a 2 mL HPLC loop. [11C]methyl triflate is passed through the loop at 40 mL/min for 11C-Raclopride and 11C-DASB, and 12 mL/min for 11C-PBR28. The reaction mixtures are purified using various specified preparative HPLC columns (Luna NH2 column for RAC and PBR, Luna CN for DASB) and aqueous ethanol eluents (20 mM NH4OAc in 15%, 20% and 80% ethanol for RAC, PBR and DASB, respectively). For 11C-Raclopride and 11C-PBR28, the products collected from HPLC are formulated with USP saline to 5% ethanol for injection. For 11C-DASB, the product collected from HPLC is diluted with water and loaded onto a C18 Sep-Pak. After washing with sterile water, the final product is eluted by 0.5 mL USP ethanol and 9.5 mL USP saline for injection. Results All three compounds have radiochemical yields of 25-45% with radiochemical purities greater than 95% and specific activities over 5 Ci/mmol. The preparative HPLC systems used here enable elution of the labeled compounds while retaining their precursors, thus avoiding contamination of products with precursors. The chemical purities of all products are significantly improved. Conclusions We have developed fully automated productions of three radiopharmaceuticals using ethanol as the organic solvent for cleaning, synthesis, purification and reformulation. By using ethanol as the only organic solvent, residual solvent analysis can be avoided and the overall production time can be reduced, while better yields and specific activities are obtained. In addition, the reversal of retention order of product and precursor from preparative HPLC improves chemical purity of the final product" @default.
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- W2228493699 date "2012-05-01" @default.
- W2228493699 modified "2023-09-23" @default.
- W2228493699 title "Improvement of C-11 radiopharmaceutical production using only ethanol as the organic solvent" @default.
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