41877-17-2Relevant academic research and scientific papers
Preparation method and application of salbutamol impurity
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Paragraph 0005; 0082-0084, (2021/06/22)
The invention discloses a preparation method and application of a salbutamol impurity. The preparation method adopts the following process route of taking 2-acetoxy-5-(2-bromoacetyl) benzyl acetate (ABBA) as an initial raw material, and firstly reacting w
Hydroxybenzothiophene ketones are efficient pre-mRNA splicing modulators due to dual inhibition of Dyrk1A and Clk1/4
Schmitt, Christian,Miralinaghi, Parisa,Mariano, Marica,Hartmann, Rolf W.,Engel, Matthias
supporting information, p. 963 - 967 (2014/12/10)
Dysregulated usage of pre-mRNA splicing sites contributes to the progression of cancer, neurodegenerative diseases, and viral infections. Serine/arginine-rich (SR) proteins play major roles in the splice site recognition and are largely regulated by phosp
Improved alkylation and product stability in phosphotriester formation through quinone methide reactions with dialkyl phosphates
Bakke, Brian A.,McIntosh, Matthias C.,Turnbull, Kenneth D.
, p. 4338 - 4345 (2007/10/03)
Investigating reactions of functionalized p-quinone methides continues to advance our design of a reagent being developed for controlled, in situ modification of DNA via phosphodiester alkylation. Previously reported investigations of p-quinone methides derived from catechols allowed for trapping of isolable trialkyl phosphates for characterization and mechanistic information. However, lactone formation with these derivatives required long reaction times, resulting in an unfavorable mixture of trialkyl phosphate and hydrolysis products. To enhance the rate and efficacy of trialkyl phosphate formation and trapping, a phenol derived p-quinone methide has been designed to enforce a conformation favoring lactonization of the dialkyl phosphate alkylated intermediate. The relative rates of phosphodiester alkylation and subsequent trapping of the phosphotriester adduct have been examined by UV and 1H NMR analysis for p-quinone methide precursor 1 and the corresponding control, 1′. The incorporation of a methyl group at the meta-position of 1 (relative to 1′) significantly improves the rate of lactionization to provide a much higher yield of the desired product, lactonized phosphotriester 5. The control reaction with 1′ afforded only a minor amount of the corresponding lactonized trialkyl phosphate 5′.
Synthesis and Structure-Activity Relationships among α-Adrenergic Receptor Agonists of the Phenylethanolamine Type
Leclerc, Gerard,Bizec, Jean Claude,Bieth, Nicole,Schwartz, Jean
, p. 738 - 744 (2007/10/02)
Nineteen arylethanolamine derivatives related to norepinephrine were prepared and tested for α-adrenergic stimulant activity.In one series the analogues possess a p-hydroxy function, while the meta position is substituted by methyl, ethyl, isopropyl, cyclohexyl, fluoro, chloro, iodo, carboxy, carbomethoxy, and methylsulfamido groups.The other series is meta hydroxylated with the para position substituted by the same groups.The influence of these groups upon the α-adrenergic activity is discussed, and the compounds are compared to octopamine, normetanephrine,norepinephrine, and norphenylephrine.It has been found that the introduction of an isopropyl, cyclohexyl, and fluoro group in the meta position of octopamine improves its affinity by three, five, and six times, respectively, whereas when these groups are introduced in the para position of norphenylephrine their effects are always detrimental.The most active compound, α-(aminomethyl)-(4-fluoro-3-hydroxyphenyl)methanol (44), has about one-hundreth the affinity and the same intrinsic activity as norepinephrine.
