530141-58-3

Upstream product

• 530141-56-1 6-(2,4-dihydroxybenzoyl)-2-chromanone 
• 96-41-3 Cyclopentanol 
• 137-43-9 Cyclopentyl bromide 
• 6342-77-4 2-methoxy-benzenepropanoic acid 
• 55001-09-7 methyl 3-(2-methoxyphenyl)propanoate 
• 91-52-1 2,4 dimethoxybenzoic acid 
• 39828-35-8 2,4-dimethoxybenzoyl chloride 

Downstream Products

• 530141-72-1 T-5224 
• 530141-60-7 methyl 3-[2-hydroxy-5-(2-hydroxy-4-cyclopentyloxybenzoyl)phenyl]propionate 

Relevant academic research and scientific papers

Synthesis technology of C-Fos/AP-1 inhibitor

The invention belongs to the technical field of pharmaceutical synthesis and especially relates to a synthesis technology of a C-Fos/AP-1 inhibitor. Starting from cheap raw materials 2,4-dimethoxybenzoic acid and 2-methoxyphenylpropionic acid, acid chloride is prepared by using thionyl chloride, and a Friedel-Crafts acylation reaction is carried out under the catalysis of aluminium trichloride soas to obtain a coupled product; then, pyridine hydrobromide and sodium chloride are used to react at 160 DEG C for 30 minutes to complete the demethylation for synthesis of lactonic ring by one step,and the product can be directly used in the next reaction without purification; the cyclopentyl group is introduced by nucleophilic substitution; the lactone ring is opened to form methyl ester; afterpurification, a benzoisoxazolyl group is introduced by nucleophilic substitution, and a protecting group is taken off to prepare the final product T5224. The route of the invention is short, and onlythe Friedel-Crafts acylation, lactone ring opening and introduction of the benzoisoxazolyl group require the step of purification. The cost of the raw materials is low, and the reaction time of the process route is short. The synthesis technology is suitable for industrial production.

NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF

A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.