125971-58-6Relevant articles and documents
Method for synthesizing atorvastatin calcium intermediate by multi-component one-pot method
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Paragraph 0152-0179, (2020/11/23)
The invention provides a method for synthesizing an atorvastatin calcium intermediate by a multi-component one-pot method, and particularly provides a one-pot method for synthesizing 4-(4-fluorophenyl)-2-(2methylpropionyl)-3-phenyl 4-oxo-N-phenyl butyramide. The preparation method is characterized in that N-phenyl phenylpropiolamide, 4-fluorobenzaldehyde and isobutyraldehyde are synthesized by a one-pot method under the action of Cu(SbF6)2 and a Pd-ligand catalyst to obtain a target compound. The one-pot method conforms to the characteristics of green chemistry and high atom economy, and emission of three wastes and pollution factors is remarkably reduced; the reaction steps are short, and the yield (about 80-87%) is obviously higher than that of the technical scheme of the existing multi-step synthesis method; raw materials are easily available; the process operation is simple; the EHS risk is low; and the industrialized feasibility is high.
Atorvastatin key intermediate for preparing environmental protection
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Paragraph 0051-0054; 0057-0058, (2019/07/01)
The present invention provides a kind of atorvastatin key intermediate of environmental protection preparation method, the intermediate body is 4 - fluoro - alpha - [2 - methyl - 1 - oxygen propyl] - gama - oxo - N, beta - diphenyl benzene ding amide, the method uses hydrogen peroxide oxidation of an alkali metal salt of bromide, bromine generated in-situ, brominated 4 '- fluorophenyl - 2 - acetophenone synthesis of 2 - bromo - 1 - (4' - fluoro phenyl) - 2 - acetophenone; above brominated alkali metal salt can be the recovery of the condensation reaction by-product, the obtained 2 - bromo - 1 - (4' - fluoro phenyl) - 2 - acetophenone with isobutyryl acetyl aniline under the action of the acid condensation reaction to obtain the target product, 4 - fluoro - alpha - [2 - methyl - 1 - oxygen propyl] - gama - oxo - N, beta - diphenyl benzene ding amide. When the condensation reaction to form a brominated alkali metal salt recovery, is used for the next batch 4' - fluorophenyl - 2 - acetophenone of the bromination reaction. The method epihalogenohydrine atomic access to fully recycle, greatly reduce the emission of halogen-containing waste. The utilization rate of higher than 80%, saving, full use of resources, reduce environmental pollution, truly environmental protection.
Preparation technology of atorvastatin
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, (2017/08/27)
The invention discloses preparation technology of atorvastatin. The preparation technology comprises the following steps: a first step, the reaction of phenylacetic acid and thionyl chloride is carried out in order to obtain phenylacetyl chloride; a second step, the Friedel-Crafts acylation reaction of phenylacetyl chloride and fluorobenzene is carried out under the action of catalyst, in order to obtain 4-fluorophenyl acetophenone; a third step, 4-fluorophenyl acetophenone is brominated and the brominated 4-fluorophenyl acetophenone is reacted with N-phenyl-isobutyloylacetamide in order to obtain M-4; a fourth step, a reaction is carried out for M-4 and ATS-9 in a cyclohexane, toluene or a mixed solvent of cyclohexane and toluene, pivalic acid is used for catalysis, and a condensation product is obtained. Phenylacetyl chloride and fluorobenzene are reacted in a catalytic action of zeolite molecular sieve, a complexation reaction of the catalyst and products is avoided, reaction yield is improved, and side reactions are few in order to facilitate purification; post-treatment can be carried out for excess M-4 for recycling and reusing, reaction yield is improved, mole proportion of M-4 to ATS-9 and the addition amount of pivalic acid can be adjusted, and final yield of the reaction is improved.
