Method for preparing key intermediate 3-amino-1-adamantanol of vildagliptin

Abstract

The invention relates to a method for preparing key intermediate 3-amino-1-adamantanol of vildagliptin. The 3-amino-1-adamantanol is prepared by taking low-price amantadine hydrochloride as an initial raw material and adopting a mixed acid method in which different acids are changed. The method is mainly characterized in that the rate of charge of fuming sulphuric acid, trifluoroacetic acid, nitric acid and amantadine hydrochloride in reaction and temperature and time in the reaction process are controlled, so that the yield of the product is greatly improved. In addition, the method provided by the invention further has the advantages of available raw material, low price, mild reaction condition, short time, less environmental pollution, cost reduction due to recycled solvent and the like, and is simple to operate and suitable for industrialized production.

Description

technical field

[0001] The invention belongs to the technical field of pharmaceutical engineering and relates to a preparation method of 3-amino-1-adamantanol, a key intermediate of vildagliptin. Background technique

[0002] Diabetes mellitus is a group of metabolic diseases characterized by hyperglycemia caused by defective insulin secretion or its biological action, or both. Diabetes is long-standing hyperglycemia, which leads to chronic damage and dysfunction of various tissues, especially the eyes, kidneys, heart, blood vessels, and nerves. It is a chronic disease that plagues the world. There are currently about 230 million patients worldwide, and it is estimated that the number of patients will increase to 350 million by 2025. Diabetes is the fourth leading cause of death in most countries, and if left untreated or undertreated, type 2 diabetes can lead to heart and kidney disease, blindness, and vascular and neuropathy. On September 28, 2007, Novartis announced tha...