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

B Di Giacomo, D Coletta, B Natalini, MH Ni…

文献索引:Di Giacomo, Barbara; Coletta, Donato; Natalini, Benedetto; Ni, Ming-Hong; Pellicciari, Roberto Farmaco, 1999 , vol. 54, # 9 p. 600 - 610

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被引用次数: 25

摘要

A new synthesis of carboxyterfenadine (4), based on the conversion of a α-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.