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Synthesis of the d,I-HM-PAO and formulation of nucleo-equipment for the obtention of {sup 99m} Tc-(d,I)-HM-PAO; Sintesis del d,I-HM-PAO y formulacion de nucleo-equipos para la obtencion de {sup 99m} Tc-(d,I)-HM-PAO

Abstract

Most brain imaging radiopharmaceuticals are conventional hydrophilic compounds that are excluded from entering the normal brain by an intact blood-brain barrier (BBB). Under pathologic conditions, the barrier is disrupted and radiotracer concentrates in the leisure for positive identification. {sup 99m} Tc- hexa methyl propylene amine oxime ({sup 99} {sup m} Tc-HM-PAO) is a newer-type lipophilic agent that enter the normal brain through an intact BBB. Studies with this agent offer the promise of measuring cerebral perfusion in the normal and diseased brain. In this paper we present the synthesis and Tc-99m labelling of d,I-HM-PAO. The synthesis of the ligand was carried out by condensation of two molecular equivalents of butanedione monoxime with one molecular equivalent of 1,3 propanediamine provided a bis imine intermediate, which was reduced with sodium borohydride to get the meso and d,I diastereoisomers of HM-PAO. Separation of these was achieved by fractional crystallization. {sup 99m} Tc-(d,I)HM-PAO was obtained by stannous ion reduction of Mo-99/Tc-99m generator eluate in the presence of the ligand. Complex radiochemical purity was determined by instant thin layer chromatography and paper chromatography. Finally, we obtained {sup 99m} Tc-(d,I)HM-PAO with a high radiochemical yield, in excess of 90%. However, for subsequent clinical studies the preparation  More>>
Publication Date:
Sep 15, 1991
Product Type:
Technical Report
Report Number:
MR-RF-02; INIS-MX-RI-0220
Subject:
37 INORGANIC, ORGANIC, PHYSICAL AND ANALYTICAL CHEMISTRY; DIAGRAMS; EXPERIMENTAL DATA; LABELLED COMPOUNDS; LABELLING; LIGANDS; RADIOCHEMISTRY; RADIOPHARMACEUTICALS; SYNTHESIS; TECHNETIUM 99; TECHNETIUM COMPLEXES; TIN CHLORIDES
OSTI ID:
20823420
Research Organizations:
Instituto Nacional de Investigaciones Nucleares, Ocoyoacac (Mexico)
Country of Origin:
Mexico
Language:
Spanish
Other Identifying Numbers:
TRN: MX0600277122464
Availability:
Available from INIS in electronic form
Submitting Site:
MXN
Size:
18 pages
Announcement Date:
Jan 04, 2007

Citation Formats

Lezama C, J, Ferro F, G, and Alcazar A, P. Synthesis of the d,I-HM-PAO and formulation of nucleo-equipment for the obtention of {sup 99m} Tc-(d,I)-HM-PAO; Sintesis del d,I-HM-PAO y formulacion de nucleo-equipos para la obtencion de {sup 99m} Tc-(d,I)-HM-PAO. Mexico: N. p., 1991. Web.
Lezama C, J, Ferro F, G, & Alcazar A, P. Synthesis of the d,I-HM-PAO and formulation of nucleo-equipment for the obtention of {sup 99m} Tc-(d,I)-HM-PAO; Sintesis del d,I-HM-PAO y formulacion de nucleo-equipos para la obtencion de {sup 99m} Tc-(d,I)-HM-PAO. Mexico.
Lezama C, J, Ferro F, G, and Alcazar A, P. 1991. "Synthesis of the d,I-HM-PAO and formulation of nucleo-equipment for the obtention of {sup 99m} Tc-(d,I)-HM-PAO; Sintesis del d,I-HM-PAO y formulacion de nucleo-equipos para la obtencion de {sup 99m} Tc-(d,I)-HM-PAO." Mexico.
@misc{etde_20823420,
title = {Synthesis of the d,I-HM-PAO and formulation of nucleo-equipment for the obtention of {sup 99m} Tc-(d,I)-HM-PAO; Sintesis del d,I-HM-PAO y formulacion de nucleo-equipos para la obtencion de {sup 99m} Tc-(d,I)-HM-PAO}
author = {Lezama C, J, Ferro F, G, and Alcazar A, P}
abstractNote = {Most brain imaging radiopharmaceuticals are conventional hydrophilic compounds that are excluded from entering the normal brain by an intact blood-brain barrier (BBB). Under pathologic conditions, the barrier is disrupted and radiotracer concentrates in the leisure for positive identification. {sup 99m} Tc- hexa methyl propylene amine oxime ({sup 99} {sup m} Tc-HM-PAO) is a newer-type lipophilic agent that enter the normal brain through an intact BBB. Studies with this agent offer the promise of measuring cerebral perfusion in the normal and diseased brain. In this paper we present the synthesis and Tc-99m labelling of d,I-HM-PAO. The synthesis of the ligand was carried out by condensation of two molecular equivalents of butanedione monoxime with one molecular equivalent of 1,3 propanediamine provided a bis imine intermediate, which was reduced with sodium borohydride to get the meso and d,I diastereoisomers of HM-PAO. Separation of these was achieved by fractional crystallization. {sup 99m} Tc-(d,I)HM-PAO was obtained by stannous ion reduction of Mo-99/Tc-99m generator eluate in the presence of the ligand. Complex radiochemical purity was determined by instant thin layer chromatography and paper chromatography. Finally, we obtained {sup 99m} Tc-(d,I)HM-PAO with a high radiochemical yield, in excess of 90%. However, for subsequent clinical studies the preparation has to be done a few minutes before application because our product has a low stability. (Author)}
place = {Mexico}
year = {1991}
month = {Sep}
}