Total chemical synthesis of PSMA-617: an API for prostate cancer endotherapeutic applications

IF 1.4 3区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR
Kalangattu Sundaran Ajish Kumar, Anupam Mathur
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引用次数: 0

Abstract

Synthesis of PSMA-617, a peptide based ligand used in the preparation of nuclear medicine, 177Lu-PSMA-617, for the treatment of prostate cancer, is demonstrated in 6 steps, starting from appropriately protected amino acid building blocks. A solution phase Boc-strategy was adopted for the synthesis of peptide, wherein deprotection of carbamate group using HCl (g), was employed as the key step. The synthesis furnished PSMA-617 in purity >99.5 % as confirmed by HPLC analysis. ESI-MS and NMR analysis supported the structural integrity of the compound. The synthesized ligand was radiolabelled using 177Lu to generate the desired radiopharmaceutical, 177Lu-PSMA-617, in radiochemical purity >98 %, as revealed by radio HPLC and TLC analysis. This establishes its potential as a nuclear medicine for therapeutic application.
PSMA-617 的全化学合成:用于前列腺癌内治疗的原料药
从适当保护的氨基酸结构单元开始,通过 6 个步骤合成了 PSMA-617(一种用于制备治疗前列腺癌的核医学 177Lu-PSMA-617 的多肽配体)。肽的合成采用了溶液相 Boc 策略,其中关键步骤是使用 HCl (g) 对氨基甲酸酯基团进行脱保护。经 HPLC 分析证实,合成的 PSMA-617 纯度为 99.5%。ESI-MS 和 NMR 分析证实了该化合物结构的完整性。使用 177Lu 对合成的配体进行放射性标记,生成了所需的放射性药物 177Lu-PSMA-617,放射性 HPLC 和 TLC 分析表明其放射化学纯度为 98%。这证明了它作为治疗用核药的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Radiochimica Acta
Radiochimica Acta 化学-核科学技术
CiteScore
2.90
自引率
16.70%
发文量
78
审稿时长
6 months
期刊介绍: Radiochimica Acta publishes manuscripts encompassing chemical aspects of nuclear science and technology.
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