40732-91-0Relevant articles and documents
Synthesis and biological evaluation of α- and β-hydroxy substituted amino acid derivatives as potential mGAT1–4 inhibitors
Andre?, Janina C.,B?ck, Michael C.,H?fner, Georg,Wanner, Klaus T.
, p. 1321 - 1340 (2020/05/25)
In this study, we report the synthesis and biological evaluation of a variety of α- and β-hydroxy substituted amino acid derivatives as potential amino acid subunits in inhibitors of GABA uptake transporters (GATs). In order to ensure that the test compounds adopt a binding pose similar to that presumed for related larger GAT inhibitors, lipophilic residues were introduced either at the amino nitrogen atom or at the alcohol function. Several of the synthesized compounds were found to exhibit similar inhibitory activity at the GAT subtypes mGAT2, mGAT3, and mGAT4, respectively, as compared with the reference N-butylnipecotic acid. Hence, these compounds might serve as starting point for future developments of more complex GAT inhibitors.
Synthesis method of gamma-phthalimido-alpha-hydroxybutyrate serving as methoxy kanamycin drug intermediate
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Paragraph 0014; 0015, (2016/11/24)
A synthesis method of gamma-phthalimido-alpha-hydroxybutyrate serving as a methoxy kanamycin drug intermediate comprises steps as follows: 0.14-0.16 mol of phthalic anhydride, 0.12 mol of L-gamma-hydroxyamino-alpha-hydroxybutyrate and 80-90 ml of a cyclohexane solution are added to a reaction container provided with a distillation device, the stirring speed is controlled to be 110-130 rpm, the solution temperature is increased to 85-90 DEG C, the temperature of the solution is increased to 105-110 DEG C after 30-40 min, reduced pressure distillation is performed for 4-5 h, brown transparent melts are obtained, cooled and cured, and brown solids are obtained; the brown solids are added to 400 ml of a potassium chloride solution, the temperature of the solution is increased to 60-70 DEG C, molecular sieves are decolored, an oxalic acid solution is added until pH of the solution is 2-3, solids are separated out, subjected to suction filtration, washed with a saline solution, dewatered with a dewatering agent and recrystallized in acetonitrile, and gamma-phthalimido-alpha-hydroxybutyrate is obtained; the mass percentage of the cyclohexane solution is 80%-85%, and the pressure for reduced pressure distillation is 1.6-1.7 kPa.
Circular dichroism of 3-hydroxy-2-pyrrolidone
Ringdahl,Craig
, p. 731 - 733 (2007/10/02)
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