Preparation method of octahydrocyclopenta[c]pyrrole carboxylic acid derivative

A technology of octahydrocyclopentyl and pyrrole carboxylic acid, applied in the production of bulk chemicals, organic chemistry, etc., can solve the problems of low yield, long route, and difficulty in large-scale production, and achieve short synthesis route and high yield Effect
CN102167680AInactive Publication Date: 2011-08-31ACME BIOPHARMA
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ACME BIOPHARMA
Publication Date
2011-08-31
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a preparation method of an octahydrocyclopenta[c]pyrrole carboxylic acid derivative. The method comprises the following steps: octahydrocyclopenta[c]pyrrole protected by N is used as raw material, one of tetrahydrofuran, methyl tert-butyl ether and dioxane is used as solvent, chiral organic ligand is added to react with lithium alkylide for 2-3 hours at -50 DEG C to -78 DEG C, then the reaction product reacts with carbon dioxide or ethyl chloroformate to obtain the octahydrocyclopenta[c]pyrrole carboxylic acid derivative. The preparation method of the octahydrocyclopenta[c]pyrrole carboxylic acid derivative has short synthetic route and high yield and can be used to realize mass production successfully.
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Description

technical field

[0001] The invention relates to a preparation method of a pharmaceutical intermediate, in particular to a preparation method of an octahydrocyclopentyl[c]pyrrole carboxylic acid derivative. Background technique

[0002] Since the hepatitis C (HCV) virus was discovered in 1989, there have been approximately 170 million viral hepatitis C patients worldwide, and 3 to 4 million new cases each year, with HCV type 1 infection as the main infection, accounting for 70%. Hepatitis C is mainly transmitted by blood. The global average infection rate is 3%, and the infection rate in China is about 3.2%. There are about 40 million hepatitis C antibody positive people in China (1b, 2a). Hepatitis C is easy to become chronic, and if it is not treated, the conversion rate is as high as 75% to 85%. After 20 to 30 years of hepatitis C infection, 10% to 20% will develop liver cirrhosis; after 30 years of hepatitis C infection, 1 to 3% will develop liver cancer. According to s...

Claims

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