Fully automated synthesis of PET TSPO radioligands [11C]DAA1106 and [18F]FEDAA1106

• Published in: Applied radiation and isotopes Vol. 70; no. 6; pp. 965 - 973
• Main Authors: Wang, Min, Gao, Mingzhang, Zheng, Qi-Huang
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.06.2012
• Subjects: [11C]DAA1106; [18F]FEDAA1106; Acetamides - chemical synthesis; Automation; Carbon Radioisotopes - chemistry; Contrast Media - chemical synthesis; Fluorine Radioisotopes - chemistry; Isotope Labeling - instrumentation; Isotope Labeling - methods; Phenyl Ethers - chemical synthesis; Positron emission tomography (PET); Positron-Emission Tomography - methods; Radiopharmaceuticals - chemical synthesis; Radiosynthesis; Robotics - instrumentation; Robotics - methods; Translocator protein 18 kDa (TSPO); [18F]FEDAA1106; Translocator protein 18kDa (TSPO); Positron emission tomography (PET); Automation; [11C]DAA1106; Radiosynthesis
• ISSN: 0969-8043; 1872-9800
• DOI: 10.1016/j.apradiso.2012.03.011

[11C]DAA1106 was prepared by O-[11C]methylation of DAA1123 with [11C]CH3OTf and NaH in CH3CN at 80°C and isolated by HPLC combined with SPE purification in 60–70% decay corrected radiochemical yield. [18F]FEDAA1106 was synthesized by the nucleophilic substitution of tosyloxy-FEDAA1106 in DMSO with K[18F]F/Kryptofix 2.2.2 at 140°C and isolated by HPLC combined with SPE purification in 30–60% decay corrected radiochemical yield. The specific activity for [11C]DAA1106 and [18F]FEDAA1106 was 370–740GBq/μmol and 37–222GBq/μmol at EOB, respectively. ► Fully automated syntheses of [11C]DAA1106 and [18F]FEDAA1106 have been developed. ► Simplified solid-phase extraction (SPE) method was employed in radiosynthesis. ► Syntheses of DAA1106, FEDAA1106 and their precursors have been improved.