329941-91-5

Upstream product

• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 161622-05-5 3-fluoro-5-(trifluoromethyl)benzoic acid 
• 171243-30-4 3-fluoro-5-trifluoromethylbenzoyl chloride 

Downstream Products

• 329941-92-6 (5-chloro-2-methoxyphenyl)[3-fluoro-5-(trifluoromethyl)phenyl]methanone 
• 329941-93-7 (5-chloro-2-hydroxyphenyl)[3-fluoro-5-(trifluoromethyl)phenyl]methanone 
• 675139-67-0 [4-chloro-2-(3-fluoro-5-trifluoromethylbenzoyl)phenoxy]acetyl chloride 
• 329946-87-4 [4-chloro-2-(3-fluoro-5-trifluoromethylbenzoyl)phenoxy]acetic acid 
• 675139-66-9 ethyl [4-chloro-2-(3-fluoro-5-trifluoromethylbenzoyl)phenoxy]acetate 
• 1364740-54-4 C₂₂H₁₃ClF₅NO₃ 
• 1364740-36-2 C₂₄H₁₃ClF₅NO₄ 

Relevant academic research and scientific papers

Practical synthesis of a benzophenone-based NNRT inhibitor of HIV-1

A convergent synthesis of NNRTI 1 is described. The key step involves a direct coupling of acid chloride 4 with Grignard reagent 11 in the presence of bis[2-(N,N-dimethylamino)ethyl] ether that moderates the reactivity of the Grignard reagent to give benzophenone 7. An efficient 2-step process for the preparation of 2-fluoro-3-methyl-4-aminobenzoic acid (3) is also described.

Benzoic acid derivatives as non nucleoside reverse transcriptase inhibitors

Compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against HIV. In particular, the compounds are

BENZOPHENONES AS INHIBITORS OF REVERSE TRANSCRIPTASE

The present invention includes benzophenone compounds (I) which are useful in the treatment of HIV infections.

Novel Benzophenones as Non-nucleoside Reverse Transcriptase Inhibitors of HIV-1

GW4511, GW4751, and GW3011 showed IC50 values ≤2 nM against wild type HIV-1 and 10 nM against 16 mutants. They were particularly potent against NNRTI-resistant viruses containing Y181C-, K103N-, and K103N-based double mutations, which account for a significant proportion of the clinical failure of the three currently marketed NNRTIs. The antiviral data together with the favorable pharmacokinetic data of GW4511 suggested that these benzophenones possess attributes of a new NNRTI drug candidate.