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Hydroxy Bupropion

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Origin: China

Cas No: 357399-43-0

Specification: 99%min

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Supply Ability: 100 mt/month

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  • Products Specification
  • Product Description

  • Property

    CAS No.: 357399-43-0 Formula: C13H18ClNO2 Molecular Weight: 255.74100

    Description

    Hydroxybupropion (code name BW 306U), or 6-hydroxybupropion, is the major active metabolite of the antidepressant and smoking cessation drug bupropion. It is formed from bupropion by the liver enzyme CYP2B6 during first-pass metabolism. With oral bupropion treatment, hydroxybupropion is present in plasma at area under the curve concentrations that are as many as 16–20 times greater than those of bupropion itself, demonstrating extensive conversion of bupropion into hydroxybupropion in humans. As such, hydroxybupropion is likely to play a very important role in the effects of oral bupropion, which could accurately be thought of as functioning largely as a prodrug to hydroxybupropion.
    Compared to bupropion, hydroxybupropion is similar in its potency as a norepinephrine reuptake inhibitor (IC50 = 1.7 µM) (and likely also acts as a norepinephrine releasing agent, similarly to bupropion), but is substantially weaker as a dopamine reuptake inhibitor (IC50 = >10 µM). Like bupropion, hydroxybupropion is also a non-competitive antagonist of nACh receptors, such as α4β2 and α3β4, but is even more potent in comparison.

    Basic Info

    Chemical Name Hydroxy Bupropion
    Synonyms

    2-(3-chlorophenyl)-3,5,5-trimethylmorpholin-2-ol;

    CAS No. 357399-43-0
    Molecular Formula C13H18ClNO2
    Molecular Weight 255.74100
    PSA 41.49000
    LogP 2.60080

    Properties

    Density 1.144 g/cm3
    Boiling Point 386.574ºC at 760 mmHg
    Flash Point 187.594ºC

    Safety Info

    HS Code 2934999090

    Synthesis Route

    2-bromo-1-(3-chlorophenyl)propan-1-one+2-Amino-2-methyl-1-propanol→Hydroxy Bupropion
    1-(3-chlorophenyl)propan-1-one→Hydroxy Bupropion

    Precursor

    2-bromo-1-(3-chlorophenyl)propan-1-one
    2-Amino-2-methyl-1-propanol
    1-(3-chlorophenyl)propan-1-one

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