82857-40-7Relevant articles and documents
A convenient method for preparing enantiomerically pure norfluoxetine, fluoxetine and tomoxetine
Koenig, Thomas M.,Mitchell, David
, p. 1339 - 1342 (1994)
A convenient synthesis for enantiomers of norfluoxetine, fluoxetine and tomoxetine is described. All final products were derived from a common intermediate, 3-phenyl-3-hydroxypropylamine.
Preparation method of cefamoxetine hydrochloride
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, (2021/10/27)
The invention discloses a preparation method of tamoxidectin hydrochloride, belongs to the technical field of drug synthesis, and uses 3 - chlorine -1 - phenylpropanone as a raw material to undergo a reduction reaction. The synthesis route has the advantages of few reaction steps, mild reaction conditions,3 - simple 2 - operation, cheap -3 - and easily available raw materials, and low production cost 3 - and -1 - R-chloro - N - phenylpropanone is used as a raw material.
Preparation method of atomoxetine hydrochloride
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, (2020/06/09)
The invention belongs to the technical field of medicines, and particularly relates to a preparation method of atomoxetine hydrochloride serving as a medicine for treating attention deficit hyperactivity. According to the invention, commercially available (E)-N-methyl-3-phenyl-2-propylene-1-amine is adopted as a starting material, and addition, substitution and salification are carried out so as to prepare atomoxetine hydrochloride. The preparation method provided by the invention is simple in preparation process, simple and convenient to operate, relatively high in yield and suitable for industrial production, and can provide sufficient bulk drugs for research and development of medicines.
R-(-)-atomoxetine hydrochloride preparation method
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Paragraph 0087; 0091-0093; 0097-0099; 0103-0104; 0109, (2019/09/14)
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.
Preparation method of atomoxetine hydrochloride
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Paragraph 0041; 0044-0047, (2019/10/15)
The invention relates to the field of medicine chemistry, and provides a preparation method of atomoxetine hydrochloride. N-methyl-3-hydroxyl-benzedrine is used as an initial raw material to take an aromatic nucleophilic substitution with o-fluorotoluene; then, through (S)-racemic ethyl mandelate resolution, salt is obtained, and the atomoxetine hydrochloride is obtained. In the route, the multistep reaction uses the continuous operation; reaction post treatment extraction and chiral resolution salt forming solvents use methyl tertiary butyl ether; during the post treatment, reduced pressure concentration operation and anhydrous sodium sulfate drying steps are not used; the operation is simple; the total yield reaches 20 to 25 percent; the purity is 99.5 percent or higher; the relevant quality standard is met. The process does not have the special reaction parameter and equipment requirements; the yield is high; byproducts are few; the post treatment is simple; the reaction yield is high; the method is suitable for industrialized production.
Preparation for atomoxetine hydrochloride
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Paragraph 0023, (2019/01/05)
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
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Paragraph 0023; 0024, (2017/08/30)
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.
Method for preparing atomoxetine hydrochloride
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Paragraph 0011, (2017/05/20)
The invention belongs to the technical field of medicines, and particularly relates to a method for preparing atomoxetine hydrochloride which is a medicine for treating attention deficit hyperactivity disorder. The atomoxetine hydrochloride is made of commercially easily available intermediates 3-methylamino-1-propiophenone hydrochloride. The method includes carrying out reduction, salt decomposition, resolving, substitution and salt forming to obtain the atomoxetine hydrochloride. The method has the advantages that technologies for preparing the atomoxetine hydrochloride are simple and stable and are easy and convenient to implement, high in yield and applicable to industrial production, and sufficient raw materials can be provided for research and development of medicines.
"AN IMPROVED PROCESS FOR THE PREPARATION OF 3-ARYLOXY-3- PHENYLPROPYLAMINE AND SALT THEREOF"
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, (2015/01/16)
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.
Process for the preparation of enantiomerically pure 3-hydroxy-3-arylpropylamines and their optical stereoisomers
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Page/Page column 10, (2009/06/27)
The invention provides a process for the preparation of enantiomerically pure 3-hydroxy-3-arylpropylamines via novel semiester derivatives containing o-carboxy benzoyl group as intermediates. The 3-hydroxy-3-arylpropylamines serve as precursor for the preparation of serotonin or noradrenalin reuptake inhibitors such as duloxetine, atomoxetine, fluoxetine, nisoxetine and norfluoxetine.