• Professor Miguel Yus (Universidad de Alicante, Spain, left) and Professor Cherif Behloul (Université de Constantine, Algérie, right)


Trityl Group Deprotection from Tetrazoles

Miguel Yus and Cherif Behloul report in SYNLETT the cleavage of the trityl group from protected tetrazoles.

Indium-Mediated Cleavage of the Trityl Group from Protected 1H-Tetrazoles: C. Behloul, M. Yus and co-workers Synlett 2015, DOI: 10.1055/s-0034-1379933

1H-Tetrazoles are privileged structures in medicinal chemistry and drug discovery: they can be found in a number of bioactive compounds and drugs, and this moiety can also be used as a carboxylic group bioisosteric replacement. The 1H-tetrazole function is a key structural component of cardiovascular drugs such as sartans (losartan, valsartan, etc). The trityl group is a key protecting group in the synthesis of nitrogen-containing heterocycles, including 1H-tetrazoles. The groups of Professors Miguel Yus and Cherif Behloul have recently reported a new efficient method for cleaving the trityl group from 1H-tetrazoles, which showed excellent selectivity and orthogonality.

  • Trityl group cleavage from protected 1H-tetrazoles

"Selective cleavage of substituted N-trityl-protected tetrazoles is easily performed with indium metal and methanol under Reflux" explained Professor Yus.
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