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Method for preparing compound of ractopamine

A ractopamine and compound technology, which is applied in the field of compound preparation, can solve the problems of slow reaction rate, increased reaction time, and difficulty in completing the reaction, and achieves the effects of easy operation, simple steps and cheap raw materials

Inactive Publication Date: 2005-08-31
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Though catalytic hydrogenation is industrially achievable, there are following disadvantages: 1, need to use inflammable dangerous gas hydrogen, and safety reduces during suitability for industrialized production; 2, catalyst Raney nickel (step II) and palladium carbon (step IV) It is an extremely active reagent, especially palladium carbon, which is prone to spontaneous combustion and brings hidden dangers to industrial safety production; 3, Raney nickel and palladium carbon are prone to catalyst poisoning and deactivation; 4, Raney nickel and palladium carbon are especially the latter , is an expensive reagent, which is not conducive to the control of production costs; 5, catalytic hydrogenation requires a special reaction device; 6, according to the experimental results, when the two-step hydrogenation reaction is carried out according to the above reaction method, it is carried out well under low reaction volume, but When the amount of raw materials is increased, the reaction rate becomes slower, the reaction time is greatly increased, and the amount of catalyst required is also greatly increased; in addition, because this reaction scheme requires vigorous stirring, it is difficult to control when there are many raw materials, and a little carelessness will seriously affect the reaction. Difficult to complete, not conducive to industrialization and safe production

Method used

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  • Method for preparing compound of ractopamine
  • Method for preparing compound of ractopamine

Examples

Experimental program
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Embodiment 1

[0026] (1) Add 100g (0.61mol) of raspberry copper and 280g (2.95mol) of formamide into a 1000ml flask, mix roughly, and then add 140ml of acetic acid. React at 130°C for two hours, distill off a large amount of water, then raise the temperature to 150°C, and react for two hours. After cooling, 600ml of water was added, and extracted four times with 700ml of ethyl acetate. The ethyl acetate layer was extracted twice with 300 ml of water. Evaporate to dryness under reduced pressure to obtain a brown viscous liquid. Add 260ml of concentrated hydrochloric acid, reflux for 25min, the solution is tea green. After cooling, a large amount of white precipitate was produced, which was washed three times with 350 ml of ethyl acetate. After drying, a white powder was obtained, which was 1-methyl-3-(4-hydroxyphenyl)-propylamine hydrochloride, and the yield was 90%.

[0027] (2) Add 6.4g (0.032mol) 1-methyl-3-(4-hydroxyphenyl)-propylamine hydrochloride, 5.4g (0.025mol) ω-bromo-p-hydroxy...

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Abstract

A process for preparing the compound Laikeduoba amine from frambone and omega-bromo-p-hydroxyacetophenone includes three steps. Its advantages are no need of noble metal catalyst and catalytic hydrogenation, and high output rate.

Description

technical field [0001] The invention relates to the field of pharmaceutical compounds, in particular to a preparation method of the compound. Background technique [0002] Ractopamine, the English name is ractopamine, the chemical name is 1-(4-hydroxyphenyl)-2-[1-methyl-3-(4-hydroxyphenyl)-propylamino]-ethanol, the structure is as (1) , is a phenylethanolamine cardiotonic drug developed by Eli Lilly & company in the United States, which can be used to treat congestive heart failure. In addition, it is also a "carcass growth agent" used in animal husbandry, which can greatly increase the growth rate of lean meat, and improve feed utilization and daily weight gain. Its safety to the human body has been confirmed, and it has been approved by the US FDA as a feed additive for aquaculture. [0003] [0004] Currently, the synthesis methods of ractopamine mainly include the patent of Eli Lilly & company of the United States (UK patent Application GB 2133986A; US patent 469095...

Claims

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Application Information

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IPC IPC(8): C07C213/00C07C215/60
Inventor 卜宪章古练权于志文黄世亮黄志纾
Owner SUN YAT SEN UNIV
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