Novel synthesis of pseudopeptides bearing a difluoromethyl group by Ugi reaction and desulfanylation

• Jingjing Wu,
• Hui Li and
• Song Cao

Beilstein J. Org. Chem. 2011, 7, 1070–1074, doi:10.3762/bjoc.7.123

• reported of the preparation and bioassay of pseudopeptides and peptidomimetics bearing difluoromethyl groups. For example, compound I can act as bradykinin B1 antagonist or inverse agonist and can be used in the prevention of inflammation and pain [19]. Compound II is an inhibitor of microsomal

An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

• Marcus Baumann,
• Ian R. Baxendale,
• Steven V. Ley and
• Nikzad Nikbin

Beilstein J. Org. Chem. 2011, 7, 442–495, doi:10.3762/bjoc.7.57

• structure, mutation studies have shown that the AT2 antagonists such as losartan bind to an active site located within the membrane-bound part of the receptor, which is different to that of the peptide agonist. Further studies led to the discovery of valsartan, where the imidazole ring of losartan is

• , and is part of the imidazopyridine class of pharmaceuticals. It is an agonist for the target receptor of γ-aminobutyric acid (GABA), an inhibitory neurotransmitter. Zolpidem binds to GABA receptors at the same site as typical benzodiazepines. This drug is preferred to benzodiazepines for long term use

• , Arimidex) and 5-HT1 agonist triptan drugs such as rizatriptan (76, Maxalt) which are prescribed for migraine headaches. The large scale syntheses of all these compounds use the commercially available 1,2,4-triazolyl sodium salt 258 in an alkylation reaction with the corresponding benzyl bromide derivative

Palladium- and copper-mediated N-aryl bond formation reactions for the synthesis of biological active compounds

• Carolin Fischer and
• Burkhard Koenig

Beilstein J. Org. Chem. 2011, 7, 59–74, doi:10.3762/bjoc.7.10

• A-366833, a selective α4β2 neural nicotinic receptor agonist. A new route to oxcarbazepine. Synthesis of key intermediates for norepinephrine transporter (NET) inhibitors. N-Annulation yielding substituted indole for the synthesis of demethylasterriquinone A1. Palladium-catalysed double N-arylation

Transition- metal/Lewis acid free synthesis of acyl benzothiophenes via C-C bond forming reaction

• Sarbani Pal,
• Mohammad Ashrafuddin Khan,
• P. Bindu and
• P. K. Dubey

Beilstein J. Org. Chem. 2007, 3, No. 35, doi:10.1186/1860-5397-3-35

• , Raloxifene, [2-(4-hydroxyphenyl)-6-hydroxybenzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]phenyl]-methanone hydrochloride (A, Figure 1), is representative of a class of compounds known as selective estrogen receptor modulators[1] (SERMs) that possess estrogen agonist-like actions on bone tissues and serum

8-epi-Salvinorin B: crystal structure and affinity at the κ opioid receptor

• Thomas A. Munro,
• Katharine K. Duncan,
• Richard J. Staples,
• Wei Xu,
• Lee-Yuan Liu-Chen,
• Cécile Béguin,
• William A. Carlezon Jr. and
• Bruce M. Cohen

Beilstein J. Org. Chem. 2007, 3, No. 1, doi:10.1186/1860-5397-3-1

• hallucinogenic sage Salvia divinorum,[1] is a potent and selective κ opioid receptor (KOR) agonist.[2] Because it is the first known non-nitrogenous compound to have biologically significant actions at mammalian opioid receptors, 1a enables new approaches to studies of endogenous opioid receptor systems. KOR