Preparation method of levocarnitine
A technology of recrystallization and intermediates, which is applied in the field of preparation of levocarnitine, can solve problems such as the inability to racemize enantiomers, and achieve the effect of high optical purity and high yield
A technology of recrystallization and intermediates, which is applied in the field of preparation of levocarnitine, can solve problems such as the inability to racemize enantiomers, and achieve the effect of high optical purity and high yield
CN106748843AActive Publication Date: 2017-05-31WUXI FORTUNE PHARMA
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[0023] The present invention will be described in detail below in conjunction with various embodiments, but it should be noted that these embodiments are not limitations of the present invention, and those of ordinary skill in the art can make functional, method, or structural equivalent transformations or replacements based on these embodiments. , all fall within the protection scope of the present invention.
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The invention provides a preparation method of levocarnitine. The preparation method comprises the following steps: taking epoxy chloropropane as a starting material, then carrying out amination, cyaniding and carrying out ester exchange under the action of lipase CALB to obtain corresponding chiral ester, then carrying out alkaline hydrolysis and acidification, and then removing chlorine ions under the action of strongly alkaline resin, so that the levocarnitine finished product is obtained. In the invention, acid resin is used in an ester exchange process, and recemization can be realized, so that yield and optical purity of the levocarnitine are improved.
Description
technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation method of levocarnitine. Background technique [0002] Levocarnitine, also known as L-carnitine, vitamin BT, chemical name: chemical name (R)-3-carboxy-2-hydroxy-N,N,N-trimethylpropylammonium hydroxide inner salt, is In vivo natural substance essential in mammalian energy metabolism. The chemical structural formula of L-carnitine is as follows: [0003] [0004] Levocarnitine is the only carrier for fatty acids to be transported to the mitochondria of cells. Therefore, the most important function of L-carnitine is to promote the β-oxidation of fatty acids, reduce the content of serum cholesterol and triglycerides, improve the body's tolerance, and can be used for treatment Chronic renal failure, cardiomyopathy, coronary heart disease, etc. It can also be used as an adjuvant drug for chronic liver disease, and has a certain protective effect on endotoxemia and...
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Patent Timeline
31 May 2017
Publication
CN106748843A
- IPC
- C07C227/18; C07C229/22
- CPC
- C07C67/08; C07C213/04; C07C227/18; C07C227/26; C07C253/14; C07C253/30; C07C229/22; C07C215/08
- Inventors
- 王庆林; 王涛