Synthesis of deuterium-labeled nelarabine and its active ingredient, ara-G
| Autor: | Ren Jing, Wang Qinglin, Zhao Damin, Yinsheng Zhang |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Stereochemistry
Guanine Health Toxicology and Mutagenesis Lymphoblastic Leukemia Analytical Chemistry chemistry.chemical_compound hemic and lymphatic diseases medicine Deoxyguanosine Radiology Nuclear Medicine and imaging Deuterium labeled Spectroscopy Active ingredient Chemistry Lymphoblastic lymphoma Public Health Environmental and Occupational Health food and beverages biochemical phenomena metabolism and nutrition Prodrug medicine.disease Pollution carbohydrates (lipids) Nuclear Energy and Engineering Nelarabine lipids (amino acids peptides and proteins) medicine.drug |
| Zdroj: | Journal of Radioanalytical and Nuclear Chemistry. 325:47-55 |
| ISSN: | 1588-2780 0236-5731 |
| Popis: | Nelarabine is a prodrug of the deoxyguanosine analogue, 9-β-D-arabinofuranose guanine (ara-G), which is used for the treatment of patients with T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL). For the clinical study of nelarabine and its active ingredient, ara-G, a suitable isotope-labeled internal standard was required. Effective and operationally simple methods for the synthesis of [D4]]nelarabine and [D3]ara-G were developed with high deuterium incorporation using D2O, CD3OD and NaBD4 as deuterium sources. It was found that [D3]ara-G was useful as an internal standard instead of [D4]nelarabine. Nelarabine is a prodrug of the deoxyguanosine analogue, 9-β-D-arabinofurose guanine (ara-G), which is used for the treatment of patients with T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-LBL). For the clinical study of nelarabine and its active ingredient, ara-G, a suitable isotope-labeled internal was not suitable as an internalstandard was required. Effective and operationally simple methods for the synthesis of [D4]]nelarabine and [D3]ara-G were developed with high deuterium incorporation using D2O, CD3OD and NaBD4 as deuterium sources. It was found that [D3]ara-G was useful as an internal standard instead of [D4 ]nelarabine. |
| Databáze: | OpenAIRE |
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