title: Synthesis optimization of 2-(4-N-[11C]methylaminophenyl)-6-hydroxybenzothiazole ([11C]PIB), β-amyloid PET imaging tracer for Alzheimer's disease diagnosis.
abstract: [11C]PIB is the most used amyloid plaques-specific positron-emitting radiotracers. The radiosynthesis of this compound, carried out by methylation of its precursor with [11C]methyl triflate in 2-butanone, has been improved optimizing the initial concentration and the purification method. Two HPLC methods were compared: good radiochemical yields, specific activities, and chemical purity above 98% were achieved by using as eluant acetonitrile/citrate and formulation in 10% ethanol.
authors.affiliation: Vita-Salute S. Raffaele University, Milan, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Coliva
authors.affiliation: CNR-IBFM c/o Department of Nuclear Medicine, Ospedale San Raffaele, Via Olgettina 60, 20132 Milan, Italy.
authors.forename: C
authors.initials: C
authors.lastname: Monterisi
authors.affiliation: CNR-IBFM c/o Department of Nuclear Medicine, Ospedale San Raffaele, Via Olgettina 60, 20132 Milan, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Apollaro
authors.affiliation: Nuclear Medicine Department, IRCCS Ospedale San Raffaele, Milan, Italy.
authors.forename: D
authors.initials: D
authors.lastname: Gatti
authors.affiliation: CNR-ISTM, Milan, Italy.
authors.forename: M
authors.initials: M
authors.lastname: Penso
authors.affiliation: Nuclear Medicine Department, IRCCS Ospedale San Raffaele, Milan, Italy.
authors.forename: L
authors.initials: L
authors.lastname: Gianolli
authors.affiliation: Vita-Salute S. Raffaele University, Milan, Italy; CNR-IBFM c/o Department of Nuclear Medicine, Ospedale San Raffaele, Via Olgettina 60, 20132 Milan, Italy.
authors.forename: D
authors.initials: D
authors.lastname: Perani
authors.affiliation: CNR-IBFM c/o Department of Nuclear Medicine, Ospedale San Raffaele, Via Olgettina 60, 20132 Milan, Italy; Nuclear Medicine Department, IRCCS Ospedale San Raffaele, Milan, Italy.
authors.forename: M C
authors.initials: MC
authors.lastname: Gilardi
authors.affiliation: CNR-IBFM c/o Department of Nuclear Medicine, Ospedale San Raffaele, Via Olgettina 60, 20132 Milan, Italy; Nuclear Medicine Department, IRCCS Ospedale San Raffaele, Milan, Italy. Electronic address: carpinelli.assunta@hsr.it.
authors.forename: A
authors.initials: A
authors.lastname: Carpinelli
mesh_terms: D000544:Alzheimer Disease / Q000175:diagnosis / Q000000981:diagnostic imaging* / Q000378:metabolism; D016229:Amyloid beta-Peptides / Q000378:metabolism*; D000814:Aniline Compounds; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000592:standards; D002250:Carbon Radioisotopes / Q000302:isolation & purification / Q000592:standards; D006801:Humans; D049268:Positron-Emission Tomography / Q000379:methods*; D011786:Quality Control; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000592:standards; D013844:Thiazoles
chemical_list: C475519:2-(4'-(methylamino)phenyl)-6-hydroxybenzothiazole; D016229:Amyloid beta-Peptides; D000814:Aniline Compounds; D052160:Benzothiazoles; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D013844:Thiazoles
keywords: Alzheimer's disease; Cyclotron; [11C]MeOTf; [11C]PIB; β-amyloid