A convenient method for 14C-labeling of N-(7-chloro-1- methyl-2-oxo-5-phenyl-2,3-dihydro-1Hbenzo[ e][1,4]diazepin-3-yl)thiophene-2-carboxamide as CCK-A antagonist

Subject Areas : Journal of the Iranian Chemical Research

Nader Saemian ¹ , Gholamhossein Shirvani ² , Mohsen Javaheri ³

1 - Nuclear science Research School, Nuclear Science & Technology Research Institute
2 - Nuclear science Research School, Nuclear Science & Technology Research Institute
3 - Nuclear science Research School, Nuclear Science & Technology Research Institute

Received: 2011-08-01 Accepted : 2012-03-11 Published : 2012-06-20

Keywords: Carbon-14, thiophene-2-carbonitrile, Cholecystokinin antagonist, benzodiazepin,

Abstract :

N-(7-chloro-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)thiophene-2 carboxamide-[14C-carboxy] was prepared as part of a 6-step sequence from thiophene-2-carbonitrile -[cyano-14C] as a keysynthetic intermediate which has been synthesized from 2-iodothiophene and zinc [14C]-cyanide in thepresence of tetrakis (triphenylphosphine) palladium.

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