1,8-Diazabicyclo[5.4.0]undec-7-ene (DBU) is a novel and active catalyst in promoting the methylation reaction of phenols, indoles, and benzimidazoles with dimethyl carbonate under mild conditions. Additional rate enhancement is accomplished by applying microwave irradiation. By incorporating tetrabutylammonium iodide, the same microwave reactions can be further accelerated. By combining these a...

Ethyl 2-[2-(4-nitrobenzoyl)-1H-indol-3-yl]acetate was prepared in good yield and characterized by the aza-alkylation/intramolecular Michael cascade reaction of (E)-ethyl 3-[2-(tosylamino)phenyl]acrylate with 2-bromo-4′ ′-nitroacetophenone, followed by desulfonative dehydrogenation with 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) The structure of the newly synthesized compound was determined using ...

An improved synthesis of the Cholesteryl Ester Transfer Protein inhibitor dalcetrapib is reported. The precursor disulfide was reduced (a) by Mg/MeOH or (b) by EtSH/DBU/THF. The resulting thiol was acylated (a) by a known procedure or (b) in a one-pot process. Impurities were removed (a) by dithiothreitol (DTT) or (b) by oxidation using H2O2. Dalcetrapib crystallized in space group P21/c.

The effects of endothelin-1 (ET-1) on the production of plasminogen activator inhibitor 1 (PAI-1) and tissue plasminogen activator (t-PA) by human brain-derived endothelial cells in culture were studied. At 100 nmol/L, ET-1 increased PAI-1 production by 8866% within 72 hours, and increased PAI-1 mRNA expression within 1 hour of stimulation; there was no significant effect on t-PA production. PA...

A new test is proposed for the hypothesis of uniformity on bi-dimensional supports. The procedure is an adaptation of the “distance to boundary test” (DB test) proposed in Berrendero, Cuevas, & Vázquez-Grande (2006). This new version of the DB test, called DBU test, allows us (as a novel, interesting feature) to deal with the case where the support S of the underlying distribution is unknown. T...

3,5-disubstituted-2,6-dicyanoaniline derivatives have been synthesized via the reaction of aryl methylene- and 1-arylethylidenemalonodinitriles using 1,8-diazabicyclo[5.4.0] undec-7-ene (dbu) as a  novel and highly efficient catalyst under conventional as well as microwave conditions. use of non-hazardous, inexpensive and readily available base catalyst, convenient procedure, short reaction tim...