Channelization synthesis method for key intermediate of sacubitril

A sacubitril and chemical synthesis technology, applied in the direction of organic chemistry and the like, can solve the problems of the hidden danger of explosion of raw material azodicarboxylate, the reaction of a large number of refrigerants, and the low yield, so as to eliminate the hidden danger of explosion, the production process is simple, and the yield is low. The effect of large specific surface area
CN109336804AActive Publication Date: 2019-02-15ZHEJIANG UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG UNIV OF TECH
Publication Date
2019-02-15

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Abstract

The invention discloses a channelization synthesis method for a key intermediate of sacubitril. The method comprises the following steps: (S)-1-([1,1'-biphenyl]-4-yl)-3-chloropropan-2-ol, succinimide,triphenylphosphine, ethyl azodicarboxylate and an organic solvent are mixed, the mixed solution is fed continuously into a channelization reactor for reaction, a feed liquid obtained after the reaction is fed into a quenching kettle containing an quenching liquid, a quenching reaction is performed with the quenching liquid, (R)-1-(1-([1,1'-biphenyl]-4-yl)-3-chloropropan-2-yl)pyrrolidin-2,5-dioneis prepared, and the key intermediate of sacubitril is obtained. According to the reaction process, reaction temperature, time and material proportion can be controlled precisely; the reactor has theadvantages of large specific surface area and high mass and heat transfer efficiency, precise proportion moment of the materials can be determined, heat transfer efficiency is high, and safety of a production process is guaranteed.
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Description

technical field

[0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a method for synthesizing a key intermediate of Shakubiqu through pipeline. Background technique

[0002] (R)-1-(1–([1,1'-biphenyl]-4-yl)-3-chloropropan-2-yl)pyrrolidine-2,5-dione (CAS: 1573000-36- 8), its molecular structural formula is as follows:

[0003]

[0004] (R)-1-(1-([1,1'-biphenyl]-4-yl)-3-chloropropan-2-yl)pyrrolidine-2,5-dione is a synthetic sacubitril (Sacubitril Qu) key intermediates. (R)-1-(1–([1,1'-biphenyl]-4-yl)-3-chloropropan-2-yl)pyrrolidine-2,5-dione was synthesized by Mitsunobu reaction , In the traditional batch synthesis process, the exothermic force is severe, and azodicarboxylate needs to be slowly added dropwise at 0°C. When amplifying, a large amount of refrigerant is required and the reaction is slow, and the yield is low; and the raw material azodicarboxylate is heated There is an explosion hazard when stirred vigorously...

Claims

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