Orlistat preparation method

Abstract

The present invention relates to an orlistat preparation method, which concretely comprises: dissolving (3S, 4S)-3-hexyl-4-[(R)-2-hydroxy tridecyl]-2-oxetanone, triphenyl phosphorous and N-formyl-L-leucine in tetrahydrofuran, adding diethyl azodicarboxylate in a dropwise manner under stirring, stirring overnight, taking out the organic phase, carrying out pressure reducing concentration, and carrying out silica gel column chromatography on the remaining material so as to obtain the product orlistat. The orlistat preparation method of the present invention has characteristics of simple preparation process and low production cost.

Description

technical field

[0001] The invention relates to the field of medicine preparation, in particular to a preparation method of orlistat. Background technique

[0002] Orlistat is currently the only OTC weight loss drug in the world. More than 40,000,000 people around the world have taken it and successfully lost weight. It is currently the best-selling weight loss product. It is effective for weight loss. Orlistat is a potent and long-acting specific gastrointestinal lipase inhibitor. By directly blocking the body's absorption of fat in food, once the intake of heat and fat is less than consumption, Naturally reduce body fat, so as to achieve the purpose of weight loss. It is safe to lose weight, the active ingredients do not enter the blood circulation, do not act on the central nervous system, have fewer side effects, and will not cause dizziness, palpitation, insomnia, dry mouth, etc. Because it is currently in the process of producing orlistat, the manufacturing process i...