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Titolo:
Rapid synthesis of F-18 and H-2 dual-labeled altanserin, a metabolically resistant PET ligand for 5-HT2A receptors
Autore:
Tan, PZ; Baldwin, RM; Fu, T; Charney, DS; Innis, RB;
Indirizzi:
Yale Univ, Sch Med, Dept Psychiat 116A2, W Haven, CT 06516 USA Yale Univ W Haven CT USA 06516 Dept Psychiat 116A2, W Haven, CT 06516 USA
Titolo Testata:
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
fascicolo: 5, volume: 42, anno: 1999,
pagine: 457 - 467
SICI:
0362-4803(199905)42:5<457:RSOFAH>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; ORGANIC HALIDES; C-11 MDL-100907; RADIOLIGAND; BRAIN; PALLADIUM; BINDING; SYSTEM;
Keywords:
[F-18]altanserin; PET; 5-HT2 receptor; deuterium isotope effect;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Physical, Chemical & Earth Sciences
Citazioni:
27
Recensione:
Indirizzi per estratti:
Indirizzo: Tan, PZ Yale6Univ, Sch Med, Dept Psychiat 116A2, 950 Campbell Ave, W Haven, CT 0651 Yale Univ 950 Campbell Ave W Haven CT USA 06516 , W Haven, CT 0651
Citazione:
P.Z. Tan et al., "Rapid synthesis of F-18 and H-2 dual-labeled altanserin, a metabolically resistant PET ligand for 5-HT2A receptors", J LABEL C R, 42(5), 1999, pp. 457-467

Abstract

F-18 and H-2 dual-labeled altanserin (3, [F-18]d-ALT), a novel PET tracer for 5-HT2A receptors with metabolically resistant properties, was synthesized by [F-18]fluoride displacement of the corresponding deuterated nitro precursor in 32% yield (EOB) in 108 min with radiochemical purity 95% and specific activity >1000 mCi/mu mol (EOS). The key intermediate ethyl N-(2-chloroethyl-2,2-d(2))carbamate (7 was obtained by LiAlD4 reduction of a glycine ester (93%), chlorination and carbamoylation (79%). 4-(4-Nitrobenzoyl)piperidine (13) was synthesized (60%) by improving the published coupling reaction of p-nitrophenyltrimethylstannane (10), obtained from p-iodonitrobenzeneand (CH3)(6)Sn-2 (94%), with 1-benzoylisonipecotic acid chloride (11) followed by acid hydrolysis. 13 was alkylated with 7 (82%), hydrolyzed and condensed with methyl o-isothiocyanatobenzoyate to provide with the precursor deuteronitmaltanserin (4, 75%).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 15:41:46