49 results about "Tomoxetine" patented technology

The invention provides an R-(-)-atomoxetine hydrochloride preparation method, which comprises: preparing 3-methylamino-1-phenyl-1-propanol by using 1-phenyl-2-propenyl-1-one as a starting raw material, carrying out etherification on the 3-methylamino-1-phenyl-1-propanol and o-halo toluene in an inorganic alkali environment, splitting with L-(+)-mandelic acid to obtain R-(-)-tomoxetine-S-(+)-mandelate, refining the R-(-)-tomoxetine-S-(+)-mandelate, and carrying out hydrochloride forming to obtain the R-(-)-atomoxetine hydrochloride. According to the present invention, the method eliminates theoxalate refining step so as to reduce the reaction step, has advantages of cheap and easily available raw materials, less side reactions, low toxicity of the reaction solvent, high yield, high purity,low cost and the like, and is suitable for industrial production.

The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(−)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water.

Provided are processes for preparing tomoxetine comprising reacting N-methyl-3-hydroxy-3-phenylpropylamine with dimethylsulfoxide (DMSO) and 2-fluorotoluene in the presence of an alkali base to form tomoxetine. Also provided is the conversion of said tomoxetine into atomoxetine or a pharmaceutically acceptable salt thereof.

The invention relates to a synthetic method of tomoxetine. The tomoxetine is generated by taking (E)-3-(N-methyl amino)-1-phenyl-2-propylene-1-ketone as the material through reduction and 2-benzyl halide etherification reaction. The synthetic method disclosed by the invention is simple in step, easy to operate, less in byproducts, better in yield, lower in cost and suitable for large-scale industrial production.

The invention discloses an atomoxetine hydrochloride oral solution for treating the attention deficit hyperactivity disorder, and a preparation method of the atomoxetine hydrochloride oral solution. The preparation comprises atomoxetine hydrochloride, hydroxypropyl-[beta]-cyclodextrin, pH regulating agent, preservative, essence, 50% ethyl alcohol and water. The preparation method comprises the following steps of: putting the water into a jar 1, carrying out stirring, adding the cyclodextrin, and carrying out dissolving to obtain a solution 1; putting 50% ethyl alcohol into a jar 2, carrying out stirring, adding the atomoxetine hydrochloride, and carrying out dissolving to obtain a solution 2; evenly mixing the solution 1 and the solution 2, transferring an obtained mixture into a grindingjar, carrying out grinding, adding the cyclodextrin, and after one hour, carrying out drying in an oven to obtain an intermediate 1; and putting the water in a preparation jar, adding the converted intermediate 1, sodium dihydrogen phosphate, phosphoric acid and sodium benzoate, carrying out stirring and dissolving, adding the essence, after the obtained mixture is even, measuring the pH value, controlling the pH value to 3.7-4.3, and obtaining 4.6mg/ ml of atomoxetine hydrochloride oral solution. The oral aqueous solution improves the stability of the atomoxetine hydrochloride to a high degree, and a higher social value is brought.

The invention relates to the field of medicines and specifically to a pharmaceutical composition for treating children's hyperactivity. The pharmaceutical composition for treating children's hyperactivity in the invention comprises tomoxetine hydrochloride and vitamin B6, and the mass ratio of tomoxetine hydrochloride to vitamin B6 is 1: 0.5 to 1:4; tomoxetine hydrochloride and vitamin B6 can be compounded with normal accessories to prepare a medicine for treating children's hyperactivity. According to the invention, composition of tomoxetine hydrochloride and vitamin B6 which weighs 0.5 to 4times of tomoxetine hydrochloride has a synergistic effect, can substantially enhance the upturning effect of NA, promote the development of brain nerves and stabilizing the functions of brain cells,and produces an effect of simultaneous treatment of principal and subordinate symptoms on children's hyperactivity.

The invention belongs to the technical field of medicines, particularly relates to the field of pharmacy, and more particularly relates to a tomoxetine hydrochloride oral liquid and a preparation method thereof. The tomoxetine hydrochloride oral liquid is mainly prepared from tomoxetine hydrochloride, a preservative, a pH regulator, a sweetening agent and a taste improver, wherein the taste improver is prepared from a thickening agent, mint essence and sweet orange essence. The taste improver prepared from the thickening agent, the mint essence and the sweet orange essence can significantly improve the taste of the tomoxetine hydrochloride oral liquid in the taking process, and significantly reduces the bitter taste during taking and the bitter taste of the oral cavity after taking. Meanwhile, a test verifies that the drug effect and the drug stability of an active drug are not affected by adding of the taste improver, and the quality of the tomoxetine hydrochloride oral liquid can beconsistent with that of an original drug.

The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(−)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water. In preferred embodiments, the atomoxetine hydrochloride produced is Form A.

The present invention provides enantiomerically pure (R)-(−)-tomoxetine (S)-(+)-mandelate and atomoxetine HCl. The present invention further provides enantiomerically pure (R)-(−)-tomoxetine (S)-(+)-mandelate prepared from racemic tomoxetine. The present invention also provides enantiomerically pure atomoxetine HCl prepared from (R)-(−)-tomoxetine (S)-(+)-mandelate.

The present invention relates to a propylamine derivative and its application in preparation of tomoxetine (atomoxetine raceme). Said invention also provides its chemical structure formula, and the invented preparation method is simple, and is suitable for industrial production.

The invention relates to pharmaceutical composition containing atomoxetine hydrochloride and a preparation method of the pharmaceutical composition, in particular to an atomoxetine hydrochloride oral solution preparation and a preparation method thereof. Beta-cyclodextrin and tartaric acid are combined for taste masking treatment, the atomoxetine hydrochloride oral solution preparation with good taste is prepared, the preparation method is simple, the atomoxetine hydrochloride oral solution preparation has the good taste, large quantities of sweetening agents, flavors and fragrances are not added, the toxic and side effects are reduced, the defects of poor compliance of existing atomoxetine hydrochloride preparations for children and the like are overcome, the medication compliance of children patients is improved, and the clinical medication requirement of children is met.