Synthesis of (125) I-lamivudine and (125) I-lamivudine-ursodeoxycholic acid codrug

M A Motaleb; M Abo-Kul; Samy M Ibrahim; Shokry M Saad; Muhammad Arafat

doi:10.1002/jlcr.3434

Synthesis of (125) I-lamivudine and (125) I-lamivudine-ursodeoxycholic acid codrug

J Labelled Comp Radiopharm. 2016 Sep;59(11):451-3. doi: 10.1002/jlcr.3434. Epub 2016 Aug 26.

Authors

M A Motaleb¹, M Abo-Kul², Samy M Ibrahim², Shokry M Saad³, Muhammad Arafat³

Affiliations

¹ Labelled Compounds Department, Hot Labs Centre, Atomic Energy Authority, Cairo, 13759, Egypt. mamotaleb10@yahoo.com.
² Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, 44519, Zagazig, Egypt.
³ Cyclotron Project, Nuclear Research Centre, Atomic Energy Authority, Cairo, 13759, Egypt.

PMID: 27561199
DOI: 10.1002/jlcr.3434

Abstract

The preparation of (125) I-lamivudine ((125) I-3TC) and (125) I-lamivudine-ursodeoxycholic acid codrug ((125) I-3TC-UDCA), suitable for comparative biodistribution studies, is described. The synthesis of the unlabeled precursor 3TC-UDCA proceeds in an 11.6% yield, and the radiolabelling yields for (125) I-3TC and (125) I-3TC-UDCA were 89 and 92%, respectively. The final products are radiochemically pure (greater than 98%).

Keywords: codrug; hepatitis B; iodine-125; lamivudine; ursodeoxycholic acid.

MeSH terms

Antiviral Agents / chemical synthesis*
Antiviral Agents / chemistry*
Chemistry Techniques, Synthetic
Iodine Radioisotopes / chemistry*
Lamivudine / chemical synthesis*
Lamivudine / chemistry*
Radiochemistry
Ursodeoxycholic Acid / chemistry*

Substances

Antiviral Agents
Iodine Radioisotopes
Lamivudine
Ursodeoxycholic Acid