{"title":"PSMA-617 的全化学合成:用于前列腺癌内治疗的原料药","authors":"Kalangattu Sundaran Ajish Kumar, Anupam Mathur","doi":"10.1515/ract-2023-0205","DOIUrl":null,"url":null,"abstract":"Synthesis of PSMA-617, a peptide based ligand used in the preparation of nuclear medicine, <jats:sup>177</jats:sup>Lu-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 <jats:sup>177</jats:sup>Lu to generate the desired radiopharmaceutical, <jats:sup>177</jats:sup>Lu-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.","PeriodicalId":21167,"journal":{"name":"Radiochimica Acta","volume":null,"pages":null},"PeriodicalIF":1.4000,"publicationDate":"2024-02-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Total chemical synthesis of PSMA-617: an API for prostate cancer endotherapeutic applications\",\"authors\":\"Kalangattu Sundaran Ajish Kumar, Anupam Mathur\",\"doi\":\"10.1515/ract-2023-0205\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Synthesis of PSMA-617, a peptide based ligand used in the preparation of nuclear medicine, <jats:sup>177</jats:sup>Lu-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 <jats:sup>177</jats:sup>Lu to generate the desired radiopharmaceutical, <jats:sup>177</jats:sup>Lu-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.\",\"PeriodicalId\":21167,\"journal\":{\"name\":\"Radiochimica Acta\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.4000,\"publicationDate\":\"2024-02-13\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Radiochimica Acta\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1515/ract-2023-0205\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, INORGANIC & NUCLEAR\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Radiochimica Acta","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1515/ract-2023-0205","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, INORGANIC & NUCLEAR","Score":null,"Total":0}
Total chemical synthesis of PSMA-617: an API for prostate cancer endotherapeutic applications
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.