A new synthesis of carboxyterfenadine (fexofenadine) and its bioisosteric tetrazole analogs

B Di Giacomo; D Coletta; B Natalini; M H Ni; R Pellicciari

doi:10.1016/s0014-827x(99)00070-1

A new synthesis of carboxyterfenadine (fexofenadine) and its bioisosteric tetrazole analogs

Farmaco. 1999 Sep 30;54(9):600-10. doi: 10.1016/s0014-827x(99)00070-1.

Authors

B Di Giacomo¹, D Coletta, B Natalini, M H Ni, R Pellicciari

Affiliation

¹ Istituto di Chimica e Tecnologia del Farmaco, Università degli Studi, Perugia, Italy.

PMID: 10555262
DOI: 10.1016/s0014-827x(99)00070-1

Abstract

A new synthesis of carboxyterfenadine (4), based on the conversion of a alpha-halo-alkylarylketone into the corresponding substituted 2-arylalkanoic ester, is described. The enantioselective synthesis of its two bioisosteric tetrazole analogs together with preliminary biological results are reported.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Histamine H1 Antagonists / chemical synthesis*
Histamine H1 Antagonists / pharmacokinetics
Humans
Magnetic Resonance Spectroscopy
Terfenadine / analogs & derivatives*
Terfenadine / chemical synthesis
Terfenadine / chemistry
Terfenadine / pharmacokinetics

Substances

Histamine H1 Antagonists
Terfenadine
fexofenadine