We describe in this study the asymmetric synthesis of radioisotope (RI)-labeled selective glucocorticoid receptor modulator. This synthesis is based on optimization of the cinchona alkaloid catalyzed addition of 6-bromoindole to ethyl trifluoropyruvate and Negishi coupling of zinc cyanide to the 6-bromoindole moiety. [¹⁴C] Labeled (-)-{4-[(1-{2-[6-cyano-1-(cyclohexylmethyl)-1H-indol-3-yl]-3,3,3...

Um procedimento melhorado para a síntese de ésteres ácido indol-2-acético em rendimentos excelentes foi obtido pela condensação de 2-halo aril aldeídos ou cetonas e isocianoacetato de etila usando líquido iônico sob irradiação de microondas controlada (100 W) a 50 C. Este método oferece um número de vantagens em termos de metodologia simples, com rendimento elevado num tempo de reação curto e e...

Abstract This work is an effort for determination of excited and ground state values dipole moments also quantum chemical computation two biologically active heterocyclic class compounds namely 3-[2-Oxo-2-(2-oxo-2H-chromen-3-yl)-ethylidene]-1,3-dihydro-indol-2-one (3OCE) 3-[2-Oxo-2-(3-oxo-3H-benzo[f]chromen-2-yl)-ethylidene]-1,3-dihydro-indol-2-one (3OBC). Redshift displayed by both the with so...

The title compound (S)-3-(3-((7-ethynyl-9H-pyrimido[4,5-b]indol-4-yl)amino)piperidin-1-yl)propanenitrile (2) was synthesized in five steps, starting from 4-chloro-7-iodo-9H-pyrimido[4,5-b]indole (3), and characterized by 1H-NMR, 13C-NMR, MS HPLC. Moreover, its structure confirmed single crystal X-ray diffraction. Pyrimido[4,5-b]indole 2 demonstrated an IC50 value of 2.24 µM a NanoBRETTM TE intr...

A series of 3-methylidene-1H-indol-2(3H)-ones substituted with a 5- or 6-pentafluorosulfanyl group has been synthesized by a Knoevenagel condensation reaction of SF5-substituted oxindoles with a range of aldehydes. The resulting products were characterized by X-ray crystallography studies and were tested for biological activity versus a panel of cell lines and protein kinases. Some exhibited si...

Centric (P2,/n) and non-centric (P2,J polymorphic pairs of biologically active 1-(4-fluorophenyl)-6,6-dimethyl-2-phenyl-1 ,5,6, 7-tetrahydro-4H-indol-4-one crystallized from different solvents have been elucidated via single crystal and powder X-ray diffraction studies, morphological observations and calorimetric measurements. C H"'O hydrogen bonding and weak intermolecular C-H" TC interactions...

The title compound, C(25)H(24)N(2)O(3) was prepared by the reaction of (Z)-2-(1H-indol-3-ylmethyl-ene)-1-aza-bicyclo-[2.2.2]octan-3-one with methyl p-(bromo-meth-yl)benzoate, under phase-transfer catalytic (PTC) conditions using triethyl-benzyl-ammonium chloride and 50% w/v aqueous NaOH solution in dichloro-methane. The crystal structure indicates the presence of a double bond with Z geometry c...