50606-33-2Relevant articles and documents
A benzo [b] thiophene preparation method and intermediate
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Paragraph 0101; 0102; 0103; 0104, (2017/08/25)
The invention provides a preparation method for benzo[b]thiophene. The preparation method comprises the following steps: substitution; ring closure; hydrolysis; decarboxylation; etc. The method effectively reduces generation of by-products, improves reaction yield, avoids usage of expensive reagents, decreases total cost and is applicable to industrial production. The invention further provides a novel compound. The novel compound is a key intermediate for preparation of benzo[b]thiophene and has a structure as shown in a formula 3 which is described in the specification. The invention also provides a preparation method for the compound 3, and the method has high yield and is simple to operate.
Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists
Zulli, Allison L.,Aimone, Lisa D.,Mathiasen, Joanne R.,Gruner, John A.,Raddatz, Rita,Bacon, Edward R.,Hudkins, Robert L.
, p. 2807 - 2810 (2012/05/20)
Optimization of a series of aminomethyl ketone diamine H3R antagonists to reduce the brain exposure by lowering the pKa, led to molecules with improved pharmacokinetic properties. Compounds 9, 19, and 25 had high affinity for human H3R and demonstrated in vivo H3R functional activity in the rat dipsogenia model. Compound 9 displayed modest wake-promoting activity in the rat EEG/EMG model.
Concerted aminolysis of diaryl carbonates: Kinetic sensitivity on the basicity of the nucleophile, nonleaving group, and nucleofuge
Castro, Enrique A.,Cubillos, Maria,Iglesias, Rocio,Santos, Jose G.
experimental part, p. 604 - 611 (2012/09/08)
The kinetics of the reactions of 4-methylphenyl, phenyl, and 4-chlorophenyl 2,4,6-trinitrophenyl carbonates (1, 2, and 3, respectively) with a series of anilines and secondary alicyclic (SA) amines has been carried out spectrophotometrically in 44 wt% ethanol-water, at 25.0°C, ionic strength 0.2 M. The BrAnsted plots (statistically corrected) for the reactions of carbonates 1-3 with anilines and SA amines were linear with slopes (βN) in the range of 0.69-0.78 and 0.45-0.48, respectively, attributed to a concerted mechanism. The negative values found for the sensitivity of log kN to the basicity of the nonleaving (βnlg) and leaving (βlg) groups are discussed. Anilines are more reactive than isobasic SA amines, probably because of the greater steric hindrance offered by the latter.