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

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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

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"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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