Literature DB >> 20099863

A rapid and efficient Sonogashira protocol and improved synthesis of free fatty acid 1 (FFA1) receptor agonists.

Elisabeth Christiansen1, Maria E Due-Hansen, Trond Ulven.   

Abstract

A protocol for rapid and efficient Pd/Cu-catalyzed coupling of aryl bromides and iodides to terminal alkynes has been developed with use of 2-(di-tert-butylphosphino)-N-phenylindole (cataCXium PIntB) as ligand in TMEDA and water. The new protocol successfully couples substrates which failed with standard Sonogashira conditions, and enables an efficient general synthetic route to free fatty acid 1 (FFA1) receptor ligands from 3-(4-bromophenyl)propionic acid.

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Year:  2010        PMID: 20099863     DOI: 10.1021/jo902533p

Source DB:  PubMed          Journal:  J Org Chem        ISSN: 0022-3263            Impact factor:   4.354


  1 in total

1.  Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.

Authors:  Elisabeth Christiansen; Steffen V F Hansen; Christian Urban; Brian D Hudson; Edward T Wargent; Manuel Grundmann; Laura Jenkins; Mohamed Zaibi; Claire J Stocker; Susanne Ullrich; Evi Kostenis; Matthias U Kassack; Graeme Milligan; Michael A Cawthorne; Trond Ulven
Journal:  ACS Med Chem Lett       Date:  2013-04-08       Impact factor: 4.345

  1 in total

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