Fluoro or difluoro-2-azabicyclo [2.2.1] heptane-3-carboxyl acid derivatives, and preparation thereof

A technology of carboxylic acid derivatives and azabicyclo, which is applied in the field of fluorinated or difluoro-2-azabicyclo[2.2.1]heptane-3-carboxylic acid derivatives and its preparation, and can solve the problem of poor metabolic stability And other issues
CN101462999AInactive Publication Date: 2009-06-24上海药明康德新药开发有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
上海药明康德新药开发有限公司
Publication Date
2009-06-24
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a fluoro or difluoro-2-diazabicyclo (2.2.1) heptane-3-carboxylic acid derivative and a preparing method thereof. A chemical structural formula is shown in the right formula. 5-hydroxyl group-2-diazabicyclo (2.2.1) heptane-3-carboxylic ester or 5-carbonyl-2-diazabicyclo (2.2.1) heptane-3-carboxylic ester is adopted for obtaining 5-fluorine-2-diazabicyclo (2.2.1) heptane-3-carboxylic ester or 5, 5-difluoro-2-diazabicyclo (2.2.1) heptane-3-carboxylic ester after the fluorination. And then carboxylic acid is obtained after hydrolysis. When the protection is drawn off, free amino compounds are obtained. By the transformation of changing protecting groups or ester groups, a target product is obtained. The derivative of the invention is mainly used as an intermediate or a structural fragment during the drug synthesis.
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Description

Technical field:

[0001] The present invention relates to fluorinated or difluoro-2-azabicyclo[2.2.1]heptane-3-carboxylic acid derivatives and preparation methods, especially 5-fluoro-2-azabicyclo[2.2.1]heptan Alkane-3-carboxylic acid derivatives and 5,5-difluoro-2-azabicyclo[2.2.1]heptane-3-carboxylic acid derivatives and preparation methods thereof. Background technique:

[0002] The bridged ring structure connects or integrates the key pharmacophore units into its rigid structure to form a molecule with a special spatial configuration and conformation, which can match the spatial structure of different biological macromolecules in the organism, and produce different biological activities or effects Many compounds have different biological activities, so they have broad application value, especially as template compounds in the process of drug research. Bridged ring compounds containing 2-azabicyclic structures have been proved by many experiments to have various biological acti...

Claims

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