848259-27-8

Usage

Uses

Used in Pharmaceutical Industry:
Pemafibrate is used as a therapeutic agent for the treatment of hyperlipidemia, a condition characterized by high levels of fats and cholesterol in the blood. It helps to regulate lipid metabolism and reduce the risk of cardiovascular diseases associated with dyslipidemia.
Additionally, Pemafibrate is used as a selective PPAR-α modulator for the treatment of combined dyslipidemia. It has shown promising results in phase 2 clinical trials with K-877, indicating its potential as a novel treatment option for patients with this condition.

Upstream product

• 907192-61-4 n-butyl (R)-2-[3-[[benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoate 
• 615-18-9 2-chloro-1,3-benzoxazole 
• 100-83-4 meta-hydroxybenzaldehyde 
• 100841-00-7 3-(4-methoxyphenoxy)propan-1-amine 
• 63815-39-4 2-(4-Methoxyphenoxy)cyanoethane 
• 150-76-5 4-methoxy-phenol 
• 95-55-6 2-amino-phenol 
• 2382-96-9 2-sulfanyl-1,3-benzoxazole 
• 692753-51-8 methyl (S)-2-chlorobutanoate 
• 907192-64-7 (S)-2-methanesulfonyloxy-butanoic acid n-butyl ester 
• 916515-10-1 (R)-3-[3-({benzoxazol-2-yl[3-(4-methoxyphenoxy)propyl]amino}methyl)phenoxy]dihydrofuran-2(3H)-one 
• 848260-89-9 3-({benzoxazol-2-yl[3-(4-methoxyphenoxy)propyl]amino}methyl)phenol 
• 909272-20-4 n-butyl (R)-2-[3-[N-[3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy]butyrate 
• 907192-65-8 (S)-2-p-toluenesulfonyloxy-butanoic acid n-butyl ester 

Relevant academic research and scientific papers

A practical synthesis of the PPARα agonist, (R)-K-13675, starting from (S)-2-hydroxybutyrolactone

A practical synthesis of optically pure PPARα agonist, (R)-K-13675, is described. This process is based on the use of (S)-2-hydroxybutyrolactone, which can be transformed into the requisite n-butyl (S)-2-hydroxybutanoate in an efficient manner. A key reaction is the etherification between the phenol and n-butyl (S)-2-trifluoromethanesulfonyloxybutanoate to give the phenyl ether in excellent yield without loss of optical purity.

PROCESSES FOR PRODUCTION OF OPTICALLY ACTIVE PPAR-ACTIVATING COMPOUNDS AND INTERMEDIATES FOR PRODUCTION THEREOF

The invention provides a process for producing an optically active butyric acid compound and a production intermediate therefor at high yield and high purity. The present invention provides a process for producing Compound (6), including reacting Compound (1) with optically active 2-trifluoromethanesulfonyloxybutyrolactone (2a) in the presence of a base or reacting optically active 2-hydroxybutyrolactone (2b) under Mitsunobu reaction conditions, to thereby form Compound (3); reacting Compound (3) with an alcohol and a halogenating agent, to thereby form Compound (4) ; dehalogenating Compound (4), to thereby form Compound (5); and de-esterifying Compound (5).

Enantioselective synthesis of the PPARα agonist (R)-K-13675 via (S)-2-hydroxybutyrolactone

Enantioselective synthesis of enantiomerically pure PPARα agonist (R)-K-13675 can be achieved starting from (S)-2-hydroxybutyrolactone. An important intermediate, 2-(aryloxy)butyrolactone, was prepared by reaction of the phenol with (S)-2-hydroxybutyrolactone in excellent yield without loss of enantiomeric purity using the Mitsunobu reaction, followed by conversion into the 2-(aryloxy)butanoic acid via the 2-(aryloxy)-4-iodobutanoate by cleavage of the lactone on exposure to iodotrimethylsilane, followed by hydrogenolysis and hydrolysis. Georg Thieme Verlag Stuttgart.

Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor α agonists

A combination of benzoxazole, phenoxyalkyl side chain, and phenoxybutyric acids was identified as a highly potent and selective human peroxisome proliferator-activated receptor α (PPARα) agonist. The synthesis, structure-activity relationship (SAR) studies, and in vivo activities of the representative compounds are described.

PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE PPAR-ACTIVATING COMPOUND AND INTERMEDIATE OF THE SAME

A process for obtaining a compound (1) and an intermediate thereof in high yield and high optical yield is provided. A process for producing a compound (4), the process including reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1), the process including reacting a compound (2) with a compound (3) in the presence of a base to yield a compound (4) and then deesterifying the compound (4). wherein R represents an alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 8 carbon atoms.

OPTICALLY ACTIVE PPAR-ACTIVATING COMPOUND INTERMEDIATE AND METHOD FOR PRODUCING SAME

The present invention provides a production intermediate for compound (A-1) and a method for producing the intermediate at high yield and high optical yield. The present invention provides a method for producing compound (3) characterized in that compound

PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE PPAR-ACTIVATING COMPOUND AND INTERMEDIATE OF THE SAME

A process for producing a compound (4) comprising the step of reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1) comprising the step of reacting a compound (2) with a compound (3) in the prese

PPAR-activating compound and pharmaceutical composition comprising the compound

A compound represented by the following formula (1): Or a salt thereof; and therapeutic durgs containing the compound. The compound selectively activates PPARα.