Practical syntheses of DOTAGA-DBCO and DFO-DBCO, strained alkyne pre-cursors to radioimmunoconjugates for targeted alpha therapy

Autor:	Zachary S. Sales, Neelakandha Mani, Aaron T. Herrmann
Rok vydání:	2022
Předmět:	History Azides Immunoconjugates Polymers and Plastics Organic Chemistry Clinical Biochemistry Pharmaceutical Science Cyclams Biochemistry Industrial and Manufacturing Engineering Cyclization Alkynes Drug Discovery Molecular Medicine Business and International Management Molecular Biology
Zdroj:	Bioorganicmedicinal chemistry. 73
ISSN:	1464-3391
Popis:	We describe practical methods to prepare DOTAGA-DBCO and DFO-DBCO from commercially available starting materials. DOTAGA-DBCO is available in five steps from cyclen with a 33 % overall yield at gram scale. Our synthesis of DFO-DBCO also proceeds in five steps from commercially available starting materials. These bifunctional molecules possess chelating functionality for the binding of medically important radiometals and a strained alkyne suitable for Huisgen cyclization with an azide. These syntheses represent an important step toward improved radioimmunoconjugates for imaging and therapeutic applications.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::effe5f4a4721f8bd1c599b39f454ad83 https://pubmed.ncbi.nlm.nih.gov/36126444 Zobrazit plný text záznamu Full Text from ScienceDirect