Atomoxetine hydrochloride powder Raw Materials CAS 82248-59-7

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Uses and synthesis of Atomoxetine hydrochloride powder

Atomoxetine hydrochloride powder is a white or light white solid, soluble in water (27.8 mg/ml). Atomoxetine hydrochloride is a hydrochloride form of the nervous system drug tomoxetine, an adrenal transmitter reuptake inhibitor, and Atomoxetine hydrochloride is used to treat attention deficit and hyperactivity disorder. Tomoxetine is a selective norepinephrine reuptake inhibitor (SNRI) with a structure similar to fluoxetine.

Applications/Functions of Atomoxetine hydrochloride powder

1. Atomoxetine hydrochloride powder is indicated for the treatment of ADHD in children and adolescents.
2. Atomoxetine hydrochloride enhances the flipping effect of norepinephrine, thereby improving ADHD symptoms and indirectly promoting cognitive completion and concentration.
3. Atomoxetine hydrochloride is mainly used to treat ADHD in children and adolescents. The drug can be taken once before or after breakfast, or it can be taken twice a day, morning and evening. Generally, 0.5-1.2 mg/kg per day. The drug also has certain adverse reactions, such as constipation, dry mouth, nausea, insomnia, etc.but the symptoms are relatively mild and generally tolerated by patients. It is contraindicated for narrow-angle glaucoma or those who are taking drugs such as phenylcypromine. The drug needs to be purchased in the hospital with a doctor's prescription and used under the guidance of a doctor. It is mainly used to treat ADHD in children and adolescents.

Effect of Atomoxetine hydrochloride powder

1. Improve attention deficit

Atomoxetine hydrochloride selectively inhibits norepinephrine reuptake and increases the concentration of neurotransmitters in the prefrontal cortex, thereby enhancing the patient's concentration and ability to perform tasks continuously. Clinical studies have shown that it can reduce the low learning efficiency of children and adolescents due to distraction.

2. Control hyperactivity and impulse

The drug acts on the central nervous system, regulates the functions of the basal ganglia and limbic system, and effectively relieves behavioral manifestations such as restlessness and random interruptions. Its mechanism of action is different from that of traditional central stimulants, and the improvement of hyperactivity symptoms is gradual and continuous.

3. Regulate emotions

For patients with concomitant mood swings, atomoxetine hydrochloride can reduce symptoms such as irritability and emotional outbursts by balancing neurotransmitter levels. Some studies have confirmed that its effect on emotional regulation helps improve patients' social function and quality of life.

4. Reduce comorbid symptoms

About 30%-40% of patients with attention deficit hyperactivity disorder have anxiety disorders. While treating the core symptoms, this drug can relieve the accompanying comorbid symptoms such as anxiety and depression by regulating the noradrenergic system of the locus coeruleus.

5. Reduce drug dependence

As a non-central nervous system stimulant drug, atomoxetine hydrochloride does not have the risk of addiction, and long-term use is not likely to cause drug dependence. Its metabolic pathway does not involve the dopaminergic system, and is more suitable for patients who need long-term treatment.

Physicochemical Property of Atomoxetine hydrochloride powder

Tomoxetine hydrochloride is a white or light white solid, soluble in water (27.8 mg/ml).

Synthesis method of Atomoxetine hydrochloride powder

Using ethyl benzoyl acetate as the starting material, bakers yeast was used for biocatalytic asymmetric reduction to obtain a chiral alcohol intermediate with a single configuration, and then atomoxetine hydrochloride was obtained through 6 steps of amidation, LiAlH4 reduction, Boc protection of amino group, Mitsunobu reaction and removal of Boc protection group.

This route involves the biocatalytic chiral reduction of baker’s yeast. This reduction method has certain stereoselectivity, but it cannot obtain a single configuration product. The optical purity of the obtained product is low, and the final product contains about 15% S type. In addition, the price of biological enzymes is high, which is not suitable for industrial production. Using LiAlH4 to reduce carbonyl in subsequent reactions has a high risk factor and is difficult to prepare industrially.

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