905089-29-4Relevant academic research and scientific papers
Structural studies of β-turn-containing peptide catalysts for atroposelective quinazolinone bromination
Metrano,Abascal,Mercado,Paulson,Miller
supporting information, p. 4816 - 4819 (2016/04/09)
We describe herein a crystallographic and NMR study of the secondary structural attributes of a β-turn-containing tetra-peptide, Boc-Dmaa-d-Pro-Acpc-Leu-NMe2, which was recently reported as a highly effective catalyst in the atroposelective bromination of 3-arylquinazolin-4(3H)-ones. Inquiries pertaining to the functional consequences of residue substitutions led to the discovery of a more selective catalyst, Boc-Dmaa-d-Pro-Acpc-Leu-OMe, the structure of which was also explored. This new lead catalyst was found to exhibit a type I′ β-turn secondary structure both in the solid state and in solution, a structure that was shown to be an accessible conformation of the previously reported catalyst, as well.
Highly enantioselective Michael Addition of α-Substituted Cyano Ketones to β,γ-unsaturated α-keto esters using bifunctional thiourea-tertiary amine catalysts: An easy access to chiral dihydropyrans
Zhao, Sheng-Li,Zheng, Chang-Wu,Wang, Hai-Feng,Zhao, Gang
supporting information; experimental part, p. 2811 - 2816 (2010/03/05)
An asymmetric Michael addition of α-substituted cyano ketones to β,γ-unsaturated α-keto esters to form chiral dihydropyrans catalyzed by a series of a-amino acid-derived thiourea-tertiary amines is presented. A novel tyrosine-derived thio-urea catalyst was identified as the optimal catalyst providing the desired product in 91-95% yields and with 90-96% ee at a low catalyst loading of 2.0mol%. The utility of the reaction was exempli-fied by facile conversion of the dihydropyran prod-uct into pharmaceutically useful dihydropyridine.
1,3-Dihydro-2H-Indole-2-One Compound and Pyrrolidine-2-One Compound Fused With Aromatic Heterocycle
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Page/Page column 95, (2009/01/24)
It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective.
