General preparation method of optical-activity 3-aminopyrrolidine, 3-alkyl amino piperidine and derivatives thereof

Abstract

The invention relates to a general preparation method of optical-activity 3-aminopyrrolidine, 3-alkyl amino piperidine and derivatives thereof by using compounds with optical activity as an initial raw material. The compounds can be simply expressed in the following molecular structure shown in the specification, wherein n is 1, 2 or 3, R1 or R2 can independently present a hydrogenous or amino-group protection group, and * presents a chiral centre with optical activity and can be R configuration or S configuration. The 3-aminopyrrolidine, 3-alkyl amino piperidine and derivatives thereof, which have optical activity, are generally used for synthesizing chiral medicaments or pesticides in the development and the production of medicaments. The invention has the advantages of cheap and easily obtainable raw materials, simple and convenient process operation, high safety, low cost and little environmental pollution and is suitable for industrial production.

Description

technical field The invention relates to the technical field of preparation of chiral drugs and their optically active intermediates, in particular to a general preparation method for optically active 3-aminopyrrolidine, 3-aminopiperidinane and their derivatives. Background technique Optically active 3-aminopyrrolidine and its derivatives are key intermediates in the synthesis of chiral drugs or pesticides. For example, patent WO2004013097 describes their application in the synthesis of Vinylpyrrolidone-Cephaloridine drugs. These compounds have highly effective antibacterial activity, especially antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa. In the patent US4854418, they are used as important intermediates for the synthesis of quinolone antibacterial drugs, and quinolone compounds are well known to have strong antibacterial properties against Gram-negative bacteria. Optically active 3-aminopiperidinane and i...

AI Technical Summary

Problems solved by technology

The first step of the method involves kinetic resolution, wasting a lot of starting material

In summary, in the existing method for synthesizing 3-aminopyrrolidine, 3-aminopiperidinane and derivatives thereof, there are various deficiencies, such as expensive raw materials, harsh reaction conditions, The final product yield is low, etc.

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