Synthesis of [allyl-2,3-3H]-MN-9201

• Published in: Journal of labelled compounds & radiopharmaceuticals Vol. 41; no. 9; pp. 785 - 789
• Main Authors: Wu, Dezhu, Huang, Wenlin, Wang, Wen, Mei, Qibing
• Format: Journal Article
• Language: English
• Published: Chichester John Wiley & Sons, Ltd 01.09.1998; Wiley
• Subjects: 3-3H]-MN-9201; [Allyl‐2,3‐3H]‐MN‐9201; Allyl-2; Biochemical Research Methods; Biochemistry & Molecular Biology; Biological and medical sciences; Cardiovascular system; Chemistry; Chemistry, Analytical; Chemistry, Medicinal; Contrast media. Radiopharmaceuticals; Life Sciences & Biomedicine; Medical sciences; Miscellaneous; MN-9201; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Physical Sciences; Science & Technology; synthesis; tritium addition; synthesis; MN-9201; [allyl-2,3-H-3]-MN-9201; BINDING-SITES; Tritium addition; Nitro compound; Catalytic reaction; Radiolabelling; Calcium antagonist; Benzenic compound; Tritium; Dihydropyridine derivatives; Palladium; Hydrogen Isotopes; Chemical synthesis; Tritiation
• ISSN: 0362-4803; 1099-1344
• DOI: 10.1002/(SICI)1099-1344(1998090)41:9<785::AID-JLCR133>3.0.CO;2-D

Key step of the synthesis of calcium antagonist MN‐9201 was the cyclizing addition of the allyl‐3‐amino‐crotonate onto methyl 2‐[(3‐nitrophenyl) methylene]‐3‐oxobutanoate. It was then used to synthesize [Allyl‐2,3‐3H]‐MN‐9201 by the catalytic addition of tritium gas. Its radiochemical purity and specific activity were 98% and 2.1 TBq/mmol, respectively. © 1998 John Wiley & Sons, Ltd.