107674-34-0

Upstream product

• 42142-52-9 3-methylamino-1-phenylpropan-1-ol 
• 95-52-3 2-Fluorotoluene 
• 144-62-7 oxalic acid 
• 63940-51-2 (+/-)-atomoxetine 

Downstream Products

• 83113-55-7 (R)-tomoxetine (S)-(+)-mandelate 
• 872996-05-9 (S)-tomoxetine (S)-(+)-mandelate 
• 63940-51-2 (+/-)-atomoxetine 
• 1027094-45-6 (R)-atomoxetine oxalate 

Relevant academic research and scientific papers

Preparation for atomoxetine hydrochloride

The invention belongs to the technical field of medicine, and particularly relates to a method for preparing atomoxetine hydrochloride with an N-methyl-3-phenoxy-benzenepropanamine content of less than 0.2%. The atomoxetine hydrochloride is a first non-excitatory drug used for treatment of attention deficit hyperactivity disorder in children and a high-selectivity norepinephrine reuptake inhibitor, has very low affinity with other neurotransmitters and does not induce a tic syndrome or increase movement disorders; and the N-methyl-3-phenoxy-benzenepropanamine is a impurity of an atomoxetine hydrochloride process and very difficult to remove by refining due to structural similarity, according to an European Pharmacopoeia, the content of the N-methyl-3-phenoxy-benzenepropanamine is not higher than 0.3, and the method disclosed by the invention can effectively control the content of the N-methyl-3-phenoxy-benzenepropanamine in the product, and improve quality of the medicine.

Preparation of atomoxetine hydrochloride

The invention belongs to the technical field of medicine, and more speficially relates to a preparation method of atomoxetine hydrochloride used for treating attention deficit hyperactivity disorders. According to the preparation method, commercially easily available 3-methylamino-1-phenylpropanol and o-fluorotoluene are taken as initial raw materials, and substitution reaction, chiral resolution, and salt forming reaction are carried out so as to obtain an atomoxetine hydrochloride product high in purity and stable in yield. The advantages of the preparation method are that: the reaction conditions are suitable for industrialized production, solvents can be recycled, more than one kind of solvents is used, and less environment pollution is caused.

"AN IMPROVED PROCESS FOR THE PREPARATION OF 3-ARYLOXY-3- PHENYLPROPYLAMINE AND SALT THEREOF"

The present invention relates to an industrially feasible and economically viable process for the preparation of 3-aryloxy-3-phenylpropylamine and salt of formula (I) thereof.

AN IMPROVED PROCESS FOR SYNTHESIZING HIGHLY PURE ATOMOXETINE

The present invention relates to a process for the preparation of highly pure atomoxetine of formula (I) and pharmaceutically acceptable salts thereof Formula (I) The present invention also aims at novel processes for the preparation and purification of intermediates involved in the process of the present invention.

PROCESS FOR PREPARING ATOMOXETINE HYDROCHLORIDE

The present invention relates to the process for preparing Atomoxetine hydrochloride which is a selective norepinephrine reuptake inhibitor. Atomoxetine HCl is chemically known as (-)-iV-Methyl-3-phenyl-3-(o-tolyloxy)-propylamine hydrochloride and represented by formula (I). More particularly, the invention relates to crystalline form of N-methyl-3-phenyl-3-(o- tolyloxy) propylamine oxalate (here in after referred as "(±) Atomoxetine Oxalate"), which is an useful intermediate for the synthesis of Atomoxetine hydrochloride.

3-ARYLOXY-3-ARYLPROPYLAMINE SYNTHESIS

A process for preparing a 3-aryloxy-3-arylpropylamine comprises reacting a 3-hydroxy-3-arylpropylamine with a substituted aryl compound, in a solvent comprising N-N-dimethylacetamide or hexamethylphosphorous triamide.

SYNTHESIS OF ATOMOXETINE HYDROCHLORIDE

(±)-Atomoxetine oxalate having crystalline Form II and a solid (±)-atomoxetine free base are useful in preparing atomoxetine hydrochloride.

Treatment of obesity with aryloxyphenylpropylamines

3-Aryloxy-3-phenylpropylamines and acid addition salts thereof are useful in blocking uptake of monoamines by brain neurons, and are thus effective in treating disorders of sleep, sexual performance, appetite, muscular function, and pituitary function.

Aryloxyphenylpropylamines in treating depression

3-Aryloxy-3-phenylpropylamines and acid additions salts thereof, useful as psychotropic agents, particularly as anti-depressants.