Synthesis of carbon‐14 labelled l,5 diaryl‐[5‐¹⁴C]‐l,2,3‐triazolines

Abstract

SummaryTwo 1,2,3-triazoline anticonvulsants, 1-(4-methylsulphone-phenyl)-5-(4-methoxyphenyl)-1,2,3-triazoline and l-(4-methylsulphone-phenyl)-5-phenyl-1,2,3-triazoline, both labelled with carbon-14 in the 5-position, have been synthesized as part of a 5-step sequence.

A Solvatochromic Model Calibrates Nitriles’ Vibrational Frequencies to Electrostatic Fields

“…As shown in Scheme 1 (synthetic methods are given in the Supplementary Information), Cu 13 CN was prepared from commercial K 13 CN with aqueous chemistry 24 ( i ). N-Fmoc-p- 13 CN-Phe ( 2 ) was prepared in moderate (40%) yield using a microwave-mediated reaction ( ii ) between the corresponding N-Fmoc-p-I-Phe ( 1 ) and Cu 13 CN.…”

1,2,3-Triazoles

“…Some triazoles work as potassium channel activators <2004FA397> , others as calcium signal transduction inhibitors <2002CLC86> . 1,5-Diaryl-Δ 2 -1,2,3-triazolines are recognized anticonvulsant agents 2003CME2081 , 2004JLR31 . Among biologically active benzotriazoles are also inactivators of the severe acute respiratory syndrome 3CL protease <2006CBO1261>, trichostatin suppressors <2003CBO397> , antagonists of the gonadotropin releasing hormone <2002BML827> , and nonpeptide inhibitors of protein tyrosine phosphatase 1B <2004BML1043> .…”

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

“…These stereoelectronic interactions can be affected by electron‐withdrawing and electron‐donating groups . A common base structural motif of the most COX‐2 selective inhibitors consists of two aryl groups linked to adjoining atoms of a central ring, which can be homocyclic or heterocyclic . One of the aryl groups is substituted in the para position with an aminosulfonyl (SO 2 NH 2 ) or a methylsulfonyl (SO 2 CH 3 ) group.…”