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HomeProduct name listDesvenlafaxine succinate

Desvenlafaxine succinate

Desvenlafaxine succinate Structural

What is Desvenlafaxine succinate?

Description

Desvenlafaxine Succinate is a dual serotonin and norepinephrine reuptake inhibitor (SNRI) that was approved for the treatment of major depressive disorder (MDD) in the United States in 2008. In order to improve the efficacy and safety profile of venlafaxine, Wyeth discovered and developed one of the major metabolites of venlafaxine, namely the O-desmethyl metabolite (desvenlafaxine). Desvenlafaxine is also being developed for the treatment of moderate to severe vasomotor symptoms associated with menopause (i.e., hot flashes and night sweats) and is also in phase III clinical trials to study it’s effectiveness in treating fibromyalgia and neuropathic pain.

The Uses of Desvenlafaxine succinate

Antianxiety therapeutic

What are the applications of Application

Desvenlafaxine succinate monohydrate is an ST and SLC6A2 inhibitor

Synthesis

Desvenlafaxine has been prepared via two different routes, and both are described in the scheme. The first route involved simple demethylation of venlafaxine (67) using L-selectride in dimethoxyethane giving desvenlafaxine 68 as its free base in 91% yield. Compound 68 was then recrystallized with succinic acid in acetone/ water to give desvenlafaxine succinate (VIII) in 86% yield. An alternative method to prepare desvenlafaxine is described in the bottom portion of the scheme. 4-Benzyloxyphenylacetic acid 69 was converted to its corresponding acid chloride upon treatment with thionyl chloride and catalytic DMF in refluxing methylene chloride. The crude reaction mixture was added to a solution of dimethylamine hydrochloride and triethyl amine in methylene chloride at 5 ??C to give dimethylacetamide 70 in 90% yield. Deprotonation of 70 with LHMDS in THF at -70 ??C followed by addition of cyclohexanone gave alcohol 71 in 82% yield. Reduction of the acetamide with borane THF complex in refluxing THF produced dimethyl amine 72 in 66% yield. Catalytic hydrogenation in the presence of 20% Pd/C effected debenzylation of 72 to give desvenlafaxine free base 68 in 87% yield.

Synthesis_386750-22-7

Properties of Desvenlafaxine succinate

storage temp.  Store at +4°C
solubility  DMSO:3.0(Max Conc. mg/mL);7.51(Max Conc. mM)
form  Powder
color  White to off-white
Stability: Hygroscopic

Safety information for Desvenlafaxine succinate

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for Desvenlafaxine succinate

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AVD pharmaceuticals Pvt Ltd

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product: 386750-22-7 Desvenlafaxine Succinate 98%
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Gonane Pharma

1Y
Phone:+919819380043
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product: Desvenlafaxine Succinate 99%
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Lupin Ltd

1Y
Phone:+91-8019896181
Whatsapp: +91 8019896181
product: Desvenlafaxine Succinate Monohydrate 386750-22-7 99%
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R L Fine Chem Pvt. Ltd

1Y
Phone:+91-8042488999
product: Desvenlafaxine Succinate Monohydrate 98%
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Adroit Pharmachem Pvt. Ltd.

1Y
Phone:+91-6358748078
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Hikal Ltd.

1Y
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Atul Bioscience Ltd

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BDR Pharmaceuticals International Pvt Ltd

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