Synthesis of [S-[1-14C]Val7]VALSPODAR application of (+)/(?)-[13,14Cn]BABS and (+)/(?)-[13,14Cn]DPMGBS, part 4
| العنوان: | Synthesis of [S-[1-14C]Val7]VALSPODAR application of (+)/(?)-[13,14Cn]BABS and (+)/(?)-[13,14Cn]DPMGBS, part 4 |
|---|---|
| المؤلفون: | Y. Metz, B. Kohler, R. Voges, P. Burtscher, R. Wenger |
| المصدر: | Journal of Labelled Compounds and Radiopharmaceuticals. 43:205-216 |
| بيانات النشر: | Wiley, 2000. |
| سنة النشر: | 2000 |
| مصطلحات موضوعية: | chemistry.chemical_classification, Chemistry, Stereochemistry, Organic Chemistry, Synthon, Alkylation, Biochemistry, Isopropyl iodide, Cyclic peptide, Analytical Chemistry, chemistry.chemical_compound, Valine, Yield (chemistry), Drug Discovery, Radiology, Nuclear Medicine and imaging, Stereoselectivity, Valspodar, Spectroscopy |
| الوصف: | VALSPODAR 2, a cyclic undecapeptide anticancer drug derived from natural Cyclosporin D10, was labelled with Carbon-14 in a nine step synthesis. The sequence started from (−)-[1-14C]BABS 1a, a highly versatile two-carbon synthon for a broad spectrum of singly/multiply labelled substance classes, which after conversion to (−)-[1-14C]DPMGBS 1b and subsequent alkylation with isopropyl iodide gave e.p. N-Boc-S[1-14C]valine 7 in 46% yield. Coupling to the respective linear decapeptide P86D, followed by cyclization and selective oxidation afforded the labelled drug substance in an overall radiochemical yield of 9%. Copyright © 2000 John Wiley & Sons, Ltd. |
| تدمد: | 1099-1344 0362-4803 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::5d459f08b478032531396e0f61f70f43 https://doi.org/10.1002/(sici)1099-1344(20000315)43:3<205::aid-jlcr303>3.0.co;2-4 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi...........5d459f08b478032531396e0f61f70f43 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 10991344 03624803 |
|---|