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Kilogram-level amplification-scale production chiral biguanide catalyst synthesis method

A synthetic method and a kilogram-level technology, applied in the direction of organic chemical methods, chemical instruments and methods, physical/chemical process catalysts, etc., can solve the problems of unsuitability for industrial production, complicated operation, and inability to scale up, so as to improve synthesis efficiency and process stability , the effect of shortening the route

Pending Publication Date: 2021-07-30
CHINA-SINGAPORE INT JOINT RES INST
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Problems solved by technology

[0004] The purpose of the present invention is to overcome the above-mentioned defects in the prior art, to provide a kind of synthetic method that can produce chiral biguanide catalyst on a large scale at the kilogram level, which mainly solves the high cost and low efficiency existing in the existing BG-I synthetic method , complex operation, inability to scale up, and technical problems that are not suitable for industrial production

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  • Kilogram-level amplification-scale production chiral biguanide catalyst synthesis method
  • Kilogram-level amplification-scale production chiral biguanide catalyst synthesis method

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Embodiment Construction

[0023] In order to make the purpose, technical solutions and advantages of the embodiments of the present invention clearer, the technical solutions in the embodiments of the present invention will be clearly and completely described below in conjunction with the drawings in the embodiments of the present invention. Obviously, the described embodiments It is a part of embodiments of the present invention, but not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without creative efforts fall within the protection scope of the present invention.

[0024] Please refer to figure 2 , figure 2 The serial numbers in are only used to indicate the substance, so as to clarify the technical solution to be protected in the present invention. figure 2 Provided is a kind of synthetic method that can produce chiral biguanide catalyst on a large scale at kilogram level, and it comprises the followin...

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Abstract

The invention discloses a kilogram-level amplification-scale production chiral biguanide catalyst synthesis method, which comprises: S1, carrying out an amine alkylation reaction by using chiral ethylenediamine and benzyl bromide as raw materials to obtain chiral bis-secondary amine; s2, adding a solvent and thiophosgene into the same kettle, carrying out a thiocarbonylation reaction to obtain chiral thiourea, and carrying out pulping purification treatment on the chiral thiourea; s3, adding oxalyl chloride into the same kettle, and performing reflux reaction in a solvent to obtain chiral 2-chloroimidazoline onium salt; and s4, evaporating out the solvent in the step S3 from the original kettle, then adding piperazine into the same kettle, and carrying out amination coupling reaction to obtain a chiral biguanide salt ion pair catalyst BG-I; and according to the synthesis method, one-kettle multi-step same-kettle feeding is adopted, the production stability and safety are improved, the synthesis route is shortened, meanwhile, the traditional tedious pulping purification process is simplified, the synthesis efficiency is improved, the synthesis cost is reduced, and the method is stable in process and suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to the field of production of chiral biguanide phase-transfer catalysts, in particular to a synthesis method capable of producing chiral biguanide catalysts on a kilogram scale. Background technique [0002] Chiral biguanide salt ion-pair phase transfer catalyst (BG-I) is widely used in various asymmetric catalysis fields, and has great application potential in the fields of organic synthesis and biomedicine, especially for the development of high value-added chiral intermediates and Drugs have great help, such as: asymmetric thioether oxidation reaction (Nat.Commun., 2016, 7, 13455), asymmetric dihydroxylation reaction and carbon-based hydroxylation reaction (J.Am.Chem.Soc., 2015,137,10677), asymmetric alkylation reaction (J.Am.Chem.Soc.,2016,138,9935) and the preparation of neurological drug Armodafinil (Nat.Commun.,2016,7, 13455). E.g figure 1 Shown in: BG-I-catalyzed asymmetric thioether oxidation for the synthesis of armod...

Claims

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Application Information

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IPC IPC(8): C07D233/48B01J31/02C07C317/44C07C315/04C07C315/02
CPCC07D233/48B01J31/0251B01J31/0244B01J31/0271C07C317/44C07C315/04C07C315/02C07B2200/07
Inventor 王杨朱文昊冯开瀛陈俊丰
Owner CHINA-SINGAPORE INT JOINT RES INST
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