Atomoxetine hydrochloride

Atomoxetine Hcl(LY 139603; Tomoxetine Hcl) is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively). IC50 value: 5 nM (Ki for human NET)Target: NETAtomoxetine displays minimal affinity for a range of other neurotransmitter receptors and transporters (Ki > 1 μM). Atomoxetine is antidepressant and a commonly used non-stimulant treatment for Attention deficit hyperactivity disor

Atomoxetine hydrochloride is the hydrochloride salt of atomoxetine. It has a role as an antidepressant and an adrenergic uptake inhibitor. It contains an atomoxetine.|Atomoxetine is a selective norepinephrine reuptake inhibitor used primarily for therapy of attention deficit hyperactivity disorder. Atomoxetine has been linked to a low rate of serum aminotransferase elevations and to rare cases of acute, clinically apparent liver injury.|Atomoxetine Hydrochloride is the hydrochloride salt of atomoxetine, a phenoxy-3-propylamine derivative and selective non-stimulant, norepinephrine reuptake inhibitor with cognitive-enhancing activity. Although its precise mechanism of action is unknown, atomoxetine appears to selectively inhibit the pre-synaptic norepinephrine transporter, resulting in inhibition of the presynaptic reabsorption of norepinephrine and prolongation of norepinephrine activity in the synaptic cleft. The effect on cognitive brain function may result in improved attention and decreased impulsivity and activity levels.|A propylamine derivative and selective ADRENERGIC UPTAKE INHIBITOR that is used in the treatment of ATTENTION DEFICIT HYPERACTIVITY DISORDER.

(R)-N-methyl-3-(2-methylphenoxy)-benzenepropanamine hydrochloride:; A 3 -necked 100 ml glass reactor was flushed for 15 min with N(R)-N-methyl-3-(2-methylphenoxy)-benzenepropanamine hydrochloride:; A 3 -necked 100 ml glass reactor was flushed for 15 min with N(R)-N-methyl-3-(2-methylphenoxy)-benzenepropanamine hydrochloride:; A 3 -necked 100 ml glass reactor was flushed for 15 min with NUnder stirring and maintaining temperature between 22° C. and 25° C. by means of water bath cooling, 10.07 g (0.09945 mol) of aqueous hydrogen chloride (36percent) were dropped on 177 g (0.08648 mol) of atomoxetine base solution (n-butyl acetate). The hydrochloride then crystallized. The obtained suspension was stirred at about 25° C. for one hour. The solid was collected by filtration and washed twice with 30 ml of n-butyl acetate each time. The solid collected was dried for 18 hours at 70° C. under vacuum. Tomoxetine hydrochloride content: >99percent by HPLC assay. Weight: 25.18 g (0.08629 mol). Yield: 99.8percent. Atomoxetine hydrochloride enantiomeric ratio: R/S>99/1 (by chiral HPLC)45 g (0.110 mol) of (R)-(-)-tomoxetine (S)-(+)-mandelate were mixed under stirring with 225 ml of toluene and 225 ml of water. Keeping the temperature at about 40° C. by means of gentle heating, 21 g (about 0.16 mol) of 30percent aqueous sodium hydroxide were added. The phases were then separated. The organic phase was washed with 100 ml of 1percent aqueous sodium hydroxide, then filtered on paper and concentrated in vacuum to give 29.67 g of an oil containing 26.8 g of tomoxetine (by HPLC assay). 23.5 g of the oil were dissolved in 211 ml of ethyl acetate under stirring then, keeping temperature between 12° C. and 18° C. by means of water-ice bath cooling; gaseous hydrogen chloride was bubbled into the solution until acid reaction of litmus paper. The hydrochloride then crystallized. The obtained suspension was stirred at about 15° C. for one hour, then the solid was collected by filtration, washed with ethyl acetate and dried in vacuo. Tomoxetine hydrochloride content: >99percent by HPLC assay. Weight: 24.3 g (0.0832 mol). Yield: 95percent.

A Norepinephrine reuptake inhibitor

Molecular Weight:291.8
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:6
Exact Mass:291.1389920
Monoisotopic Mass:291.1389920
Topological Polar Surface Area:21.3
Heavy Atom Count:20
Complexity:237
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes