Pipecolinic acid preparation process based on reverse dropping

Abstract

The invention discloses a pipecolinic acid preparation process based on reverse dropping and belongs to the technical field of medicines. By adopting the pipecolinic acid preparation process based onreverse dropping, S1-S2 and S3-S7 can be implemented simultaneously, so that the lasting time of the whole preparation process can be effectively shortened; meanwhile, by adopting a dropping mode in the preparation process, a conventional mode of dropping from top to bottom is changed into a mode of dropping from bottom to top, small water domes can be formed because of instantaneous impact resulted when a liquid to be dropped is fed into a reaction kettle, and are diffused outwards and upwards, liquid convection of the dropped liquid and a reactant can be enhanced because of the water domes,thus a good mixing effect is achieved, reactions can be accelerated to a certain extent, the preparation efficiency can be improved, and compared with the mode of dropping from top to bottom, the process is capable of effectively avoiding the phenomenon that the content of the reactant is changed to a certain extent as the liquid is splashed because of water impact and is adhered to an inner wall.

Description

technical field [0001] The invention relates to the technical field of medicine, and more specifically, relates to a pipecolic acid preparation process based on reverse dropwise addition. Background technique [0002] Pipecolic acid (PA) is an important rigid cyclic non-protein amino acid, which can not only limit the conformation of polypeptides, but also serve as a multifunctional backbone in the synthesis library of different compounds, so it is widely used in many chiral Preparation of pharmaceuticals and biologically active substances. For example, the new-generation local anesthetic Ropivacaine, the antipsychotic drug Thioridazine, the immunosuppressant Rapamycin, and the antitumor antibiotic Sandramycin are all based on Pipecolic acid or its derivatives are the main raw materials. [0003] Due to the biological activity and wide application prospects of pipecolic acid and its derivatives, its synthesis has attracted the interest of many foreign researchers, and many...

AI Technical Summary

Problems solved by technology

[0004] The pipecolic acid prepared by the present invention is specifically 3-[(1,1-dimethylethyl) dimethylsiloxo]-2-aminopropyl-dimethylethyl ester-1-pipercolic acid, But because the preparation process of 3-[(1,1-dimethylethyl) dimethylsiloxo]-2-aminopropyl-dimethylethyl ester-1-pipericolic acid is extremely complicated, and its The required preparation time is extremely long, and in the entire preparation process, the chains are interlocking, and the preparation steps cannot be parallelized, so that the long-term operations required by many steps, such as dropping, stirring, etc., cannot be carried out at the same time, resulting in each step. It takes a long time, the preparation efficiency is difficult to improve, and the difficulty is difficult to reduce, which has a great impact on the preparation of the drug intermediate

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