B W Schoultz, E Arstad, J Marton, F Willoch, A Drzezga, H-J Wester, G Henriksen
{"title":"C标记氨基甲酸酯基的放射性合成及其在kappa -阿片受体示踪剂合成中的应用[j]。","authors":"B W Schoultz, E Arstad, J Marton, F Willoch, A Drzezga, H-J Wester, G Henriksen","doi":"10.2174/1874104500802010072","DOIUrl":null,"url":null,"abstract":"<p><p>(11)C-labeled carbamates can be obtained in a three-component coupling reaction of primary or secondary amines with CO(2) and (11)C-methylation reagents. [(11)C]Methyl-triflate mediated methylation of carbamino adducts provides the corresponding (11)C-labeled carbamate groups in excellent yields under mild conditions (temperatures </= 40 degrees C, 2 min reaction time). The utility of the method has been demonstrated by a highly efficient radiosynthesis of [(11)C]GR103545.</p>","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":" ","pages":"72-4"},"PeriodicalIF":0.0000,"publicationDate":"2008-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2704583/pdf/","citationCount":"14","resultStr":"{\"title\":\"A New Method for Radiosynthesis of C-Labeled Carbamate Groups and its Application for a Highly Efficient Synthesis of the Kappa-Opioid Receptor Tracer [C]GR103545.\",\"authors\":\"B W Schoultz, E Arstad, J Marton, F Willoch, A Drzezga, H-J Wester, G Henriksen\",\"doi\":\"10.2174/1874104500802010072\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>(11)C-labeled carbamates can be obtained in a three-component coupling reaction of primary or secondary amines with CO(2) and (11)C-methylation reagents. [(11)C]Methyl-triflate mediated methylation of carbamino adducts provides the corresponding (11)C-labeled carbamate groups in excellent yields under mild conditions (temperatures </= 40 degrees C, 2 min reaction time). The utility of the method has been demonstrated by a highly efficient radiosynthesis of [(11)C]GR103545.</p>\",\"PeriodicalId\":39133,\"journal\":{\"name\":\"Open Medicinal Chemistry Journal\",\"volume\":\" \",\"pages\":\"72-4\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2008-07-16\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2704583/pdf/\",\"citationCount\":\"14\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Open Medicinal Chemistry Journal\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/1874104500802010072\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Open Medicinal Chemistry Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1874104500802010072","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
A New Method for Radiosynthesis of C-Labeled Carbamate Groups and its Application for a Highly Efficient Synthesis of the Kappa-Opioid Receptor Tracer [C]GR103545.
(11)C-labeled carbamates can be obtained in a three-component coupling reaction of primary or secondary amines with CO(2) and (11)C-methylation reagents. [(11)C]Methyl-triflate mediated methylation of carbamino adducts provides the corresponding (11)C-labeled carbamate groups in excellent yields under mild conditions (temperatures = 40 degrees C, 2 min reaction time). The utility of the method has been demonstrated by a highly efficient radiosynthesis of [(11)C]GR103545.