Synthesis of (R,S)-[4-11C]baclofen via Michael addition of nitromethane labeled with short-lived 11C

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 21, 2009, Pages 6222-6224

  Kato, Koichi ^a   Zhang, Ming Rong ^a   Suzuki, Kazutoshi ^a  

^a NATIONAL INSTITUTE OF RADIOLOGICAL SCIENCES   (Japan)

Author keywords

Baclofen; GABAB; Nitro 11C methane; Positron emission tomography

Indexed keywords

BACLOFEN; BACLOFEN C 11; BORATE SODIUM; CINNAMIC ACID DERIVATIVE; HYDROLASE; METHYL 4 CHLOROCINNAMATE; NICKEL CHLORIDE; NITROMETHANE; TETRABUTYLAMMONIUM; UNCLASSIFIED DRUG;

ARTICLE; BIOTRANSFORMATION; BRAIN; CONTROLLED STUDY; DRUG INHIBITION; DRUG SYNTHESIS; HYDROLYSIS; ISOTOPE LABELING; MICHAEL ADDITION; NITRATION; RADIOASSAY; REDUCTION;

BACLOFEN; CARBON RADIOISOTOPES; GABA AGONISTS; METHANE; NITROPARAFFINS; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RECEPTORS, GABA-B;

EID: 71749107378     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.08.097     Document Type: Article

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31. 4 (19 mg) at rt. After 3 min, a 5 N NaOH aqueous solution (300 μL) was added and the resulting mixture was warmed to 80 °C. After 3 min at 80 °C, an aqueous buffer solution was added (500 μL) and the contents of the resulting mixture were analyzed by HPLC. HPLC conditions for 2: column J'sphere ODS-H80 (4.6 × 150 mm, 4 μm, YMC Co. Ltd), flow rate 0.7 mL/min, eluent 30/70 (MeOH/50 mM phosphoric acid) detector NaI scintillation, retention time 5.1 min. The peak of radioactivity of 2 corresponded with the UV absorption (254 nm) of non-labeled baclofen purchased from Sigma-Aldrich Co. Ltd.