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Online Publishing Date:
25 / 04 / 2022

 


Preparation of the 5-(4-((4-[18F] fluorobenzyl) oxy)- 3-methoxybenzyl) pyrimidine-2, -diamine as a radioligand for positron emission tomography scanning of the tyrosine kinase b/C receptor

Seyyed Hossein Hassanpour, Alireza Doroudi, Seyyedeh Zeinab Karami.


Abstract
Objective: The present research describes a new radiosynthesis of 5-(4-((4-[18F]fluorobenzyl)oxy)-3-methoxybenzyl)pyrimidine- 2,4-diamine as a potential radioligand for colony-stimulating factor 1 receptor (CSF-1R) and tyrosine kinase B/C (TrkB/C) neuroreceptors.
Methods: Radiofluorination of a boronic acid precursor followed by thermal deprotection of Boc-protecting groups avoided acidcatalyzed protodeboronation in 8.7 ± 2.8% radiochemical yield.
Results: Competitive autoradiographic binding research indicated a high unspecific binding, and that binding to TrkB/C could be blocked while binding to CSF-1R was not. In a rat model, a positron emission tomography (PET) scan indicated a moderate brain uptake and slow clearance rate.
Conclusion: Moreover, the poor pharmacokinetic features of 5-(4-((4-[18F]fluorobenzyl)oxy)-3-methoxybenzyl)pyrimidine-2,4- diamine prevented its utilization as a PET radioligand in brain scanning, but 1-pot synthesis (which is a strategy to improve the effectiveness of the chemical reaction occurring by the use of copper, 18F-fluorination, and Boc deprotection) is an approach to the radio-synthesis of PET tracers (which are sensitive to acid).

Key words: Tyrosine kinase; Colony-stimulating factor 1 receptor; 18F; Positron emission tomography


 
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How to Cite this Article
Pubmed Style

Hassanpour SH, Doroudi A, Karami SZ. Preparation of the 5-(4-((4-[18F] fluorobenzyl) oxy)- 3-methoxybenzyl) pyrimidine-2, -diamine as a radioligand for positron emission tomography scanning of the tyrosine kinase b/C receptor. Pak J Nucl Med. 2022; 12(1): 37-48. doi:10.24911/PJNMed.175-1631138374

Web Style

Hassanpour SH, Doroudi A, Karami SZ. Preparation of the 5-(4-((4-[18F] fluorobenzyl) oxy)- 3-methoxybenzyl) pyrimidine-2, -diamine as a radioligand for positron emission tomography scanning of the tyrosine kinase b/C receptor. https://www.pjnmed.com/?mno=121993 [Access: February 27, 2024]. doi:10.24911/PJNMed.175-1631138374

AMA (American Medical Association) Style

Hassanpour SH, Doroudi A, Karami SZ. Preparation of the 5-(4-((4-[18F] fluorobenzyl) oxy)- 3-methoxybenzyl) pyrimidine-2, -diamine as a radioligand for positron emission tomography scanning of the tyrosine kinase b/C receptor. Pak J Nucl Med. 2022; 12(1): 37-48. doi:10.24911/PJNMed.175-1631138374


Vancouver/ICMJE Style

Hassanpour SH, Doroudi A, Karami SZ. Preparation of the 5-(4-((4-[18F] fluorobenzyl) oxy)- 3-methoxybenzyl) pyrimidine-2, -diamine as a radioligand for positron emission tomography scanning of the tyrosine kinase b/C receptor. Pak J Nucl Med. (2022), [cited February 27, 2024]; 12(1): 37-48. doi:10.24911/PJNMed.175-1631138374


Harvard Style

Hassanpour, S. H., Doroudi, . A. & Karami, . S. Z. (2022) Preparation of the 5-(4-((4-[18F] fluorobenzyl) oxy)- 3-methoxybenzyl) pyrimidine-2, -diamine as a radioligand for positron emission tomography scanning of the tyrosine kinase b/C receptor. Pak J Nucl Med, 12 (1), 37-48. doi:10.24911/PJNMed.175-1631138374


Turabian Style

Hassanpour, Seyyed Hossein, Alireza Doroudi, and Seyyedeh Zeinab Karami. 2022. Preparation of the 5-(4-((4-[18F] fluorobenzyl) oxy)- 3-methoxybenzyl) pyrimidine-2, -diamine as a radioligand for positron emission tomography scanning of the tyrosine kinase b/C receptor. Pakistan Journal of Nuclear Medicine, 12 (1), 37-48. doi:10.24911/PJNMed.175-1631138374


Chicago Style

Hassanpour, Seyyed Hossein, Alireza Doroudi, and Seyyedeh Zeinab Karami. "Preparation of the 5-(4-((4-[18F] fluorobenzyl) oxy)- 3-methoxybenzyl) pyrimidine-2, -diamine as a radioligand for positron emission tomography scanning of the tyrosine kinase b/C receptor." Pakistan Journal of Nuclear Medicine 12 (2022), 37-48. doi:10.24911/PJNMed.175-1631138374


MLA (The Modern Language Association) Style

Hassanpour, Seyyed Hossein, Alireza Doroudi, and Seyyedeh Zeinab Karami. "Preparation of the 5-(4-((4-[18F] fluorobenzyl) oxy)- 3-methoxybenzyl) pyrimidine-2, -diamine as a radioligand for positron emission tomography scanning of the tyrosine kinase b/C receptor." Pakistan Journal of Nuclear Medicine 12.1 (2022), 37-48. Print. doi:10.24911/PJNMed.175-1631138374


APA (American Psychological Association) Style

Hassanpour, S. H., Doroudi, . A. & Karami, . S. Z. (2022) Preparation of the 5-(4-((4-[18F] fluorobenzyl) oxy)- 3-methoxybenzyl) pyrimidine-2, -diamine as a radioligand for positron emission tomography scanning of the tyrosine kinase b/C receptor. Pakistan Journal of Nuclear Medicine, 12 (1), 37-48. doi:10.24911/PJNMed.175-1631138374




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