1171823-92-9

Usage

Uses

Used in Pharmaceutical Industry:
(S)-Ethyl 3-(1-hydroxy-3-methylbutan-2-ylamino)-2-(5-bromo-2,4-dimethoxybenzoyl)acrylate is used as a pharmaceutical intermediate for the synthesis of various drugs. Its specific chemical structure and properties make it a valuable component in medicinal chemistry and drug development.
Used in Medicinal Chemistry:
(S)-ethyl 3-(1-hydroxy-3-methylbutan-2-ylamino)-2-(5-bromo-2,4-dimethoxybenzoyl)acrylate is utilized in medicinal chemistry for studying certain biological processes and for designing new pharmaceutical compounds with specific properties and activities. Its unique combination of functional groups allows for targeted modifications and enhancements in drug development.
Used in Drug Development:
(S)-Ethyl 3-(1-hydroxy-3-methylbutan-2-ylamino)-2-(5-bromo-2,4-dimethoxybenzoyl)acrylate plays a role in drug development by providing a foundation for the creation of novel pharmaceuticals. Its structural features can be manipulated to achieve desired therapeutic effects and improve the efficacy of resulting medications.

Upstream product

• 96901-91-6 5-bromo-2,4-dimethoxy-benzoyl chloride 
• 32246-20-1 5-bromo-2,4-dimethoxybenzoic acid 
• 91-52-1 2,4 dimethoxybenzoic acid 
• 2026-48-4 (S)-valinol 
• 1171823-91-8 ethyl 2-(5-bromo-2,4-dimethoxybenzoyl)-3-(dimethylamino)acrylate 
• 182056-48-0 1-(5-bromo-2,4-dimethoxyphenyl)ethan-1-one 
• 829-20-9 2',4'-dimethoxyacetophenone 
• 949014-39-5 ethyl 3-(5-bromo-2,4-dimethoxyphenyl)-3-oxopropanoate 

Downstream Products

• 949014-40-8 ethyl 2-(5-bromo-2,4-dimethoxybenzoyl)-3-((S)-1-(tert-butyldimethyl-silanyloxymethyl)-2-methylpropylamino)acrylate 
• 697761-98-1 elvitegravir 

Relevant academic research and scientific papers

Preparation method of elviravir

The invention provides a preparation method of elviravir, and belongs to the technical field of medicine preparation. According to the method, 2, 4-dimethoxybenzoic acid is used as a raw material and is sequentially subjected to a bromination reaction, an

An Improved Synthesis of Elvitegravir

An improved process for the active pharmaceutical ingredient of a new HIV integrase inhibitor elvitegravir (1) has been developed. It starts from commercially available 2,4-dimethoxyacetophenone, which is selectively halogenated into the position 5. The 5-halo acetophenones are condensed with dialkyl carbonates to give the corresponding benzoylacetates. Their treatment with N,N-dimethylformamide dimethyl acetal followed by (S)-valinol then provided the corresponding intermediate benzoyl acrylates. Cyclization to the required 1,4-dihydroquinolin-4-oxo derivatives by aromatic nucleophilic substitution of the 2-methoxy group was achieved by treatment with N,O-bis(trimethylsilyl)-acetamide, which also protected the OH group as the trimethylsilyl derivative. Finally, the Negishi coupling with 2-fluoro-3-chlorobenzylzinc bromide and the following hydrolysis provided elvitegravir (1). The preferred variant, the seven-step procedure starting from 2,4-dimethoxyacetophenone, provides elvitegravir in 29.3% yield.

A NEW PRODUCTION METHOD AND NEW INTERMEDIATES OF SYNTHESIS OF ELVITEGRAVIR

The present solution relates to an improved production method of elvitegravir of formula I, which is being clinically evaluated for treatment of HIV infection. Elvitegravir of formula I is produced via the intermediate of formula II, the preparation of which is also an object of the present solution.

PROCESS FOR PRODUCTION OF 4-OXOQUINOLINE COMPOUND

The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifi