FLUORINATION PROCESS OF ANILIDE DERIVATIVES AND BENZOTHIAZOLE FLUORINATE DERIVATIVES AS IN VIVO IMAGING AGENTS

• Main Authors: Steven Michael FAIRWAY, Nicolas LASBISTES, Lorenzo WILLIAMS, Clare Louise JONES, Bengt LANGSTROM, Farhad KARIMI, Anthony Eamon STOREY, Alexander Mark GIBSON, Robert James NAIRNE, Denis Raymond Christophe BOUVET
• Format: Patent
• Language: English; Spanish
• Published: 10.08.2016
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEAR ENGINEERING; NUCLEAR PHYSICS; NUCLEAR REACTORS; ORGANIC CHEMISTRY; PHYSICS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

The invention relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl ; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl,C6-14arylalkyl, -(CH2CH2O)q-CH3wher ein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed. La presente invención se refiere a un proceso para la preparación de un compuesto de la fórmula (I): R1 es seleccionado de C1-6alquilo, C2-6alquenilo y C2-6alquinilo; el cual comprende (I) la reacción con fluoruro, en forma adecuada [18F]fluoruro, de un compuesto correspondiente de la fórmula (II): en donde R2 es seleccionado de hidrógeno, C1-10alquilo, C1 10haloalquilo, C6-14arilo, C6-14arilalquilo, (CH2CH2O)qCH3 en donde q es un entero de 1 a 10; R1 es tal como se define para el compuesto de la fórmula (I); y R3 es un grupo de partida. También se reivindican ciertos precursores novedosos de la fórmula (II) y equipos radiofarmacéuticos que contienen dichos precursores.