<abstract xmlns="http://www.w3.org/1999/xhtml"><p> A modification of biphenylyltetrazole moiety of Losartan <italic>(A) </italic>by 3-(2-heteroaryl)-pyrazolotetrazole <italic>(B) </italic>is described. Ketone semicarbazones react with two moles of phosphorus oxychloride-dimethylformamide with the formation of 3-substituted pyrazol-4-carbaldehydes. The transformations of 3-substituted pyrazole-4- carboxaldehydes to 3-substituted pyrazole-4-nitriles were carried out by reaction of hydroxylamine in DMFA. The prepared cyano pyrazoles were converted to tetrazoles by heating with trimethylsilylazide and dibuthyltinoxide in toluene.</p></abstract>

A modification of biphenylyltetrazole moiety of Losartan (A) by 3-(2-heteroaryl)-pyrazolotetrazole (B) is described. Ketone semicarbazones react with two moles of phosphorus oxychloride-dimethylformamide with the formation of 3-substituted pyrazol-4-carbaldehydes. The transformations of 3-substituted pyrazole-4- carboxaldehydes to 3-substituted pyrazole-4-nitriles were carried out by reaction of hydroxylamine in DMFA. The prepared cyano pyrazoles were converted to tetrazoles by heating with trimethylsilylazide and dibuthyltinoxide in toluene.

3-(2-Heteroaryl)-pyrazolotetrazoles – a subunits for losartan-like structures

Institute of Organic Chemistry, Catalysis and Petrochemistry, Faculty of Chemical and Food Technology, Slovak University of Technology, Radlinského 9, 81237 Bratislava, Slovakia

Institute of Physical Chemistry and Chemical Physics, Faculty of Chemical and Food Technology, Slovak University of Technology, Radlinského 9, 812 37 Bratislava, Slovakia

Acta Chimica Slovaca

A modification of biphenylyltetrazole moiety of Losartan (A) by 3-(2-heteroaryl)-pyrazolotetrazole (B) is described. Ketone semicarbazones react with two moles...

3-(2-Heteroaryl)-pyrazolotetrazoles – a subunits for losartan-like structures

Publicado en línea: 14 dic 2012

Páginas: 220 - 224

DOI: https://doi.org/10.2478/v10188-012-0033-z

Palabras clave
Angiotensin II receptor antagonists, 3-, 4-substituted pyrazoles, tetrazoles

This content is open access.

3-(2-Heteroaryl)-pyrazolotetrazoles – a subunits for losartan-like structures

Publicado en línea: 14 dic 2012

Páginas: 220 - 224

DOI: https://doi.org/10.2478/v10188-012-0033-z

Palabras claveAngiotensin II receptor antagonists, 3-, 4-substituted pyrazoles, tetrazoles

This content is open access.

Palabras clave
Angiotensin II receptor antagonists, 3-, 4-substituted pyrazoles, tetrazoles