154801-74-8

Usage

Uses

Used in Pharmaceutical Industry:
L 743725 is used as an antiviral agent for the treatment of HIV-1 infection. It works by inhibiting the reverse transcriptase enzyme, which is crucial for the replication of the virus. This action helps to prevent the spread of the virus in the body and can slow down the progression of the disease.
Used in Research and Development:
L 743725 is also used as a research tool in the development of new antiviral drugs and therapies. Its unique mechanism of action and effectiveness against HIV-1 make it a valuable compound for studying the virus's replication process and identifying potential targets for new treatments.
Used in Clinical Trials:
L 743725 may be used in clinical trials to evaluate its safety, efficacy, and potential side effects when used as a treatment for HIV-1 infection. These trials can provide valuable information on the drug's effectiveness and help to determine the optimal dosage and treatment regimen for patients.

InChI:InChI=1/C14H9ClF3NO2/c15-9-3-4-11-10(7-9)13(14(16,17)18,21-12(20)19-11)6-5-8-1-2-8/h3-4,7-8H,1-2H2,(H,19,20)/t13-/m1/s1

Upstream product

• 177530-93-7 rac-efavirenz 
• 886371-22-8 1-(2,5-dichloro-phenyl)-2,2,2-trifluoroethanone 
• 1381993-90-3 (S)-carbamic acid cyclopropyl-(2,5-dichloro-phenyl)-trifluoromethyl-prop-2-ynyl ester 
• 1381993-88-9 (S)-2-(2,5-dichlorophenyl)-4-cyclopropyl-1,1,1-trifluorobut-3-yn-2-ol 
• 106-46-7 para-dichlorobenzene 
• 209414-27-7 (2S)-2-(2-amino-5-chlorophenyl)-4-cyclopropyl-1,1,1-trifluorobut-3-yn-2-ol 
• 154598-53-5 1-(2-amino-5-chloro-phenyl)-2,2,2-trifluoro-ethanone 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 1236354-27-0 (S)-2-(2-amino-5-chlorophenyl)-4-cyclopropyl-1,1,1-trifluorobut-3-yn-2-ol methanesulfonate 
• 6746-94-7 Cyclopropylacetylene 
• 503-38-8 trichloromethyl chloroformate 
• 75-44-5 phosgene 

Relevant academic research and scientific papers

Development and Validation of RP-Chiral HPLC Method for Determination of (R)-Enantiomer Excess Content in Efavirenz

A simple, specific, linear, accurate and precise reverse phase chiral HPLC method was developed for the separation of efavirenz enantiomers by using the Lux Amylose-2 column containing amylose tris(5-chloro-2-methyl phenyl carbamate) as a stationary phase. The mobile phase consists of 0.1 % formic acid in water and acetonitrile (55:45, v/v). The flow rate was kept at 1.0 mL/min and the detection wavelength used 252 nm and the column temperature was set at 25 oC. The limit of detection was 0.01 mg/mL and the limit of quantification was 0.04 mg/mL. The linearity calibration curve of (R)-enantiomer was shown well from the range of 0.04 mg/mL to 0.4 mg/mL. The values of the correlation coefficient were 0.999 and 0.999 for (R)-enantiomer and (S)-efavirenz, respectively. The percentage recoveries of (R)-enantiomer from efavirenz drug substance were ranged from 93.5% to 107.5%. The results demonstrated that developed RP-chiral HPLC method was simple, precise, robust and applicable for the estimation of (R)-enantiomer in efavirenz API. This method was validated in as per ICH Q2 (R1) and USP validation of compendial methods .

Eluent tolerance and enantioseparation recovery of chiral packing materials based on chitosan bis(phenylcarbamate)-(n-octyl urea)s for high performance liquid chromatography

The goal of the present work was to study the influence of the swelling of chitosan derivatives on the enantioseparation and the separation performance recovery of chiral stationary phases (CSPs) based on these derivatives. Therefore, six chitosan bis(phenylcarbamate)-(n-octyl urea)s were synthesized, which were coated on macroporous 3-aminopropyl silica gel affording new CSPs. Most of the CSPs demonstrated strong enantioseparation capability for the tested chiral compounds. The swelling capacity of the chitosan bis(phenylcarbamate)-(n-octyl urea)s in ethyl acetate, acetone and tetrahydrofuran (THF) was evaluated. Among the chitosan derivatives, the chitosan bis(3,5-dichlorophenylcarbamate)-(n-octyl urea) polymer showed the highest swelling capacity in ethyl acetate and THF. The polymer-based CSPs could be utilized with pure ethyl acetate and a normal phase containing 70% THF, but was damaged by pure THF. On the other hand, the separation performance of the damaged CSP could be recovered after it was allowed to stand for a period of time. The observations are important for the development and application of polysaccharide derivative-based CSPs.

PROCESS FOR PREPARATION OF EFAVIRENZ BY CYCLISATION

The invention disclosed a process for the preparation of the HIV drug Efavirenz, also known as DMP-266, starting from 1,4-dichlorobenzene, and its intermediates.

Process for the synthesis of chiral propargylic alcohols

A process for the synthesis of chiral propargylic alcohols.