110-73-6Relevant articles and documents
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Goldberg,Whitmore
, p. 2280 (1937)
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Further Studies on a Site-specific Hydrogen Transfer Observed in Electron Capture Negative Ion Chemical Ionization Mass Spectrometry of Hydroxyamine Pentafluoropropionate Derivatives
Low, G. K.-C.,Duffield, A. M.
, p. 595 - 599 (1985)
Further studies have demonstrated that the site-specific hydrogen transfer process involved in the formation of the m/z 145 anion of β-hydroxyamine pentafluoropropionate (PFP) derivatives observed under electron capture negative ion chemical ionization conditions occurs when the two functional groups are separated by up to five carbon atoms.Deuterium labelling has established that the site specificity, transfer of a hydrogen atom from the carbon adjacent to nitrogen to the OPFP group, is maintained in 4-amino-butan-1-ol-N,O-(PFP)2.The corresponding PFP derivatives of the N-methylaminoalkanol- (PFP)2 derivatives lack the m/z 145 species with m/z 163, -, being the base anion.Substitution of alkyl groups on the carbon adjacent to oxygen results in a diminution of the ion intensity at m/z 145 with a marked increase in the intensity of m/z 144.The formation of the m/z 145 and 144 anions is proposed to proceed through the intervention of a fluoride ion-molecule complex as outlined in Scheme 1 with the product ion distribution dependent on which of the two pathways is preferred.
Discovery of benzimidazole analogs as a novel interleukin-5 inhibitors
Boggu, Pulla Reddy,Kim, Youngsoo,Jung, Sang-Hun
, (2019/08/12)
A series of novel hydroxyethylaminomethylbenzimidazole analogs 5a-y were synthesized and evaluated for their IL-5 inhibitory activity using pro-B Y16 cell line. Among them, 2-(((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)amino)butan-1-ol (5e, 94.3% inhibition at 30 μM, IC50 = 3.5 μM, cLogP = 4.132) and 3-cyclohexyl-2-(((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)amino) propan-1-ol (5k, 94.7% inhibition at 30 μM, IC50 = 5.0 μM, cLogP = 6.253) showed the most potent inhibitory activity. The essential feature of SAR (Fig. 5) indicated that the chromenone ring can be replaced by a benzimidazole ring to maintain the inhibitory activity. In addition, the hydroxyethylaminomethyl group was suitable for the IL-5 inhibitory activity. Moreover, the hydrophobic substituents on carbon play an important role in the IL-5 inhibitory activity of these analogs. However, N-substituted analogs did not improve inhibitory activity. In addition, MTT assay of 5e and 5k with normal B lymphoblasts revealed that they had no significant effects on cell viability.
METHOD FOR PRODUCING 2-(ALKYLAMINO)ETHANOL COMPOUND
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Paragraph 0042, (2017/08/24)
PROBLEM TO BE SOLVED: To provide a method for effectively producing a 2-(alkylamino)ethanol compound from a N-alkyldiethanolamine compound. SOLUTION: A method for producing a 2-(alkylamino)ethanol compound in which a N-alkyldiethanolamine compound and an alkylamine compound are reacted under the presence of at least one metal catalyst selected from the group consisting of iron catalyst, copper catalyst, nickel catalyst, cobalt catalyst, palladium catalyst, platinum catalyst, silver catalyst, gold catalyst, osmium catalyst, iridium catalyst, ruthenium catalyst, and rhodium catalyst is provided. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
