Synthesis of (2-mercaptoacetyl)-L-[2- C]tryptophan as a selective metallo-β-lactamase inhibitor via [2- C]indole based on chiral pool strategy.

Metallo-beta-lactamase enzymes make bacteria resistant to a broad range of commonly used beta-lactam antibiotics. Several thiol derivatives of L-amino acids have been shown their inhibitory effects against the metallo-β-lactamase IMP-1. In this study, (2-mercaptoacetyl)-L-tryptophan as a new inhibitor of metallo-β-lactamases labeled with carbon-14 in the 2-position of the indole ring was prepared from [2- C]indole as a key synthetic intermediate based on chiral pool strategy.

Preparation of 1-fluoro-4-methyl-9H-[carbonyl-(14) C]thioxanthen-9-one and amine derivatives.

9H-Thioxanthen-9-ones are an important class of compound and are a common heterocyclic scaffold in biologically active and medicinally significant compounds. In this paper the synthesis of 1-fluoro-4-methyl-9H-thioxanthen-9-one and some amine derivatives labeled with carboxyl-14 is described.

Synthesis of the olanzapine labeled by carbon-14.

Olanzapine is one of the most widely used antipsychotic drugs, which acts as an antagonist for multiple neurotransmitter receptor sites. 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno [2,3-b][1,5] benzodiazepine (Olanzapine) labeled with carbon-14 in the four positions has been synthesized as part of a three-step sequence from 2-amino-5-methylthiophene-3-carbonitrile-[carbonitrile-(14) C].

Synthesis of 2-(methylsulfonyl)-5-(4-(methylsulfonyl) phenyl)-4-phenyl-1H-[5-(14)C]imidazole, a selective COX-2 inhibitor, via asymmetrical benzoins.

4,5-Diarylimidazoles labeled with carbon-14 in the 5-position of the imidazole ring were prepared as a part of three-step sequence from 2-hydroxy-1-(4-(methylthio)phenyl)-2-phenyl[1-(14) C]ethanone as a key synthetic intermediate which has been synthesized from potassium [(14) C]cyanide.

Synthesis of a series of carbon-14 labeled tetrahydropyrido[4,3-d]pyrimidin-4(3H)-ones.

A series of tetrahydropyrido[4,3-d]pyrimidin-4(3H)-ones labeled with carbon-14 in the 2-position of pyrimidinone moiety were prepared as part of a 3-step sequence from benz[amidino-(14) C]amidine hydrochloride as a key synthetic intermediate.

Synthesis of carbon-14 analogue of 1,5 diaryl-5-[14C]-1,2,3-triazoles.

Two 1,2,3-triazole anticonvulsants, 1-(4-methylsulfone-phenyl)-5-(4-methyl-phenyl)-1,2,3-triazole and 1-(4-methylsulfone-phenyl)-5-phenyl-1,2,3-triazole, both labeled with carbon-14 in the 5-position were prepared from para-tolunitrile-[cyano-14C] and benzonitrile-[cyano-14C], respectively.

Synthesis of a carbon-14 analogue of 8-chloro-11-(4-methyl-1-piperazinyl)-11-[14C]-dibenz[b,f][1,4]oxazepine.

8-Chloro-11-(4-methyl-1-piperazinyl)-dibenz[b,f][1,4]oxazepine labelled with carbon-14 in 11-position was prepared from 2-hydroxy benzonitrile-[cyano-14C].