120777-22-2Relevant articles and documents
Asymmetric biocatalytic hydrocyanation of pyrrole carboxaldehydes
Purkarthofer, Thomas,Gruber, Karl,Fechter, Martin H.,Griengl, Herfried
, p. 7661 - 7668 (2005)
The asymmetric hydrocyanation of pyrrole-2- and -3-carboxaldehydes substituted with either methyl, benzyl or phenyl in the 1-position catalyzed by the hydroxynitrile lyases from Hevea brasiliensis (HbHNL) and Prunus amygdalus (PaHNL) is reported. The products could be isolated - after O-silylation - with moderate to good enantiomeric purity although the carbonyl activity of the substrates was found to be very low, which is supported by quantum-chemical calculations. Structural effects concerning substrate size and regiochemistry are discussed considering docking calculations based on the X-ray crystal structures of the two enzymes. From these calculations one particular amino acid residue (Trp-128) in the active site of HbHNL could be identified, which plays a major role for the appropriate binding of structurally demanding carbonyl compounds.
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding
Thurkauf,Yuan,Chen,Wasley,Meade,Woodruff,Huston,Ross
, p. 4950 - 4952 (1995)
A series of 1-phenyl-3-(aminomethyl)pyrroles were prepared in two steps from aniline and their affinities for D2, D3, and D4 dopamine receptor subtypes determined. A 15-fold selectivity for cloned human D4 recep
Direct and efficient synthesis of pyrrole-3-carbaldehydes by Vilsmeier-Haack formylation of pyrroles with sterically crowded amides
Ilyin, Petrv.,Pankova, Alenas.,Kuznetsov, Mikhail A.
experimental part, p. 1353 - 1358 (2012/07/03)
A simple and convenient synthetic method to prepare N-substituted pyrrole-3-carbaldehydes by Vilsmeier-Haack formylation of pyrroles using sterically crowded formamides was developed. The dependence of the formylation regioselectivity on steric features of substrates and reagents is discussed. Georg Thieme Verlag Stuttgart · New York.
NOVEL ANTIFUNGAL AGENT COMPRISING HETEROCYCLIC COMPOUND
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Page/Page column 90, (2010/11/08)
The present invention provides an antifungal agent represented by the formula: [wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula -NH-C(=O)-, a group represented by the formula -C(=O)-NH-, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents].