2848-96-6

Usage

Uses

Used in Pharmaceutical Industry:
3-(Acetyloxy)-7-chloro-5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one is used as a potential pharmaceutical compound for its distinctive properties. The presence of multiple chlorinated and carbonylated phenyl groups may confer unique characteristics to 3-(Acetyloxy)-7-chloro-5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one, making it a candidate for further research and development in the pharmaceutical sector.
Used in Medical Research:
3-(Acetyloxy)-7-chloro-5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one is used as a subject of medical research to explore its potential applications and effects. The complex structure of 3-(Acetyloxy)-7-chloro-5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one, with its 1,4-benzodiazepine core and additional functional groups, may offer insights into new therapeutic approaches or drug development strategies.

InChI:InChI=1/C17H12Cl2N2O3/c1-9(22)24-17-16(23)20-14-7-6-10(18)8-12(14)15(21-17)11-4-2-3-5-13(11)19/h2-8,17H,1H3,(H,20,23)

Upstream product

• 64-19-7 acetic acid 
• 2894-67-9 delorazepam 
• 127-08-2 potassium acetate 
• 14405-03-9 2-chloroacetamido-2’,5-dichlorobenzophenone 
• 2958-36-3 (2-amino-5-chloro-phenyl)-(2-chloro-phenyl)-methanone 

Downstream Products

• 71107-66-9 lorazepam-α-methyl-β-phenyl-propionate 
• 82841-78-9 lorazepam-α-chloro-propionate 
• 71107-65-8 lorazepam-β-phenyl-propionate 
• 846-49-1 lorazepam 

Relevant academic research and scientific papers

New crystal form of lorazepam, preparation method and pharmaceutical applications thereof

The invention relates to a new crystal form for preparing lorazepam, a preparation method and pharmaceutical applications thereof, wherein specifically the lorazepam crystal has diffraction peaks at about 12.17 DEG, about 14.15 DEG, about 15.27 DEG, about 16.84 DEG, about 17.91 DEG and about 20.81 DEG in a powder X-ray diffraction pattern represented by a 2[theta] angle by using Cu-Kalpha radiation, for example, the crystal has diffraction peaks at about 7.93 DEG, about 9.04 DEG, about 12.17 DEG, about 14.15 DEG, about 15.27 DEG, about 16.84 DEG, about 17.91 DEG, about 20.81 DEG, about 21.44 DEG and about 26.38 DEG. The invention further provides a preparation method of the new crystal of larazepam, and pharmaceutical applications of the new crystal form. According to the invention, the prepared new crystal form for preparing lorazepam shows excellent properties defined in the specification.

Light-stabilized pharmaceutical composition, and preparation method and pharmaceutical application thereof

The invention relates to a light-stabilized pharmaceutical composition, and a preparation method and pharmaceutical application thereof. Specifically, the pharmaceutical composition comprises a lorazepam crystal and pharmaceutical adjuvants. The lorazepam crystal is radiated by Cu-K alpha. In a powder X-ray diffraction pattern expressed by an angle of 2 theta, there are diffraction peaks at approximately 12.17 degrees, approximately 14.15 degrees, approximately 15.27 degrees, approximately 16.84 degrees, approximately 17.91 degrees and approximately 20.81 degrees. For example, the crystal hasdiffraction peaks at approximately 7.93 degrees, approximately 9.04 degrees, approximately 12.17 degrees, approximately 14.15 degrees, approximately 15.27 degrees, approximately 16.84 degrees, approximately 17.91 degrees, approximately 20.81 degrees, approximately 21.44 degrees and approximately 26.38 degrees. A new crystal form and the pharmaceutical composition, which are used for preparing lorazepam and prepared by the method, exhibit excellent properties as described in the description of the invention.

Method for preparing lorazepam

The invention relates to a method for preparing lorazepam. The method comprises the following steps: subjecting a ketone substrate as shown in a formula I, glacial acetic acid, potassium acetate, potassium persulfate and iodine to a reaction under heating and stirring conditions to obtain an acetoxy substrate as shown in a formula II; dropwise adding a sodium hydroxide solution into a mixture of ethanol and the acetoxy substance as shown in the formula II, carrying out stirring to realize a complete reaction, performing filtering to obtain a filter cake, and reacting the filter cake with ethylacetate and a citric acid solution to obtain a crude lorazepam product; and crystallizing the crude lorazepam product by using ethanol and ethyl acetate in sequence. The invention further relates tothe pharmaceutical application of larazepam prepared by using the method. The larazepam is particularly used for treating or preventing anxiety, epilepsy, convulsion, sedation and hypnosis. The methoddisclosed by the invention has excellent technical effects as described in the specification.

Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloro-quinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives

A series of 4-aryl-6-chloro-quinolin-2-ones and 5-aryl-7-chloro-1,4-benzodiazepine were synthesized and assayed for their in vitro anti-hepatitis B virus activities and cytotoxicities for the first time. Some of the tested compounds were active against HBsAg and HBeAg secretion in Hep G2.2.15 cells. Compound 5c showed IC50 of 0.074 and 0.449 mM on HBsAg and HBeAg secretions, respectively, which were 10 times higher than that of its analog 4c and led to better selective index (SI) values (SI = 23.2 and 3.4, respectively).

Efficient synthesis of 3-hydroxy-1,4-benzodiazepines oxazepam and lorazepam by new acetoxylation reaction of 3-position of 1,4-benzodiazepine ring

Simple, efficient, and scalable syntheses of 3-hydroxy-1,4-benzodiazepines, oxazepam (1), and lorazepam (2) were developed. The syntheses are based on the new acetoxylation reaction of the 3-position of the 1,4-benzodiazepine ring. The reaction involves iodine (20-50 mol %)-catalyzed acetoxylation in the presence of potassium acetate (2 equiv) and potassium peroxydisulfate (1-2 equiv) as a stoichiontetric oxidant affording the corresponding 3-acetoxy-1,4- benzodiazepines in good-to-high yields. The latter were converted by selective saponification to 3-hydroxy-1,4-benzodiazepines of very high purity (>99.8%) in an overall yield of 83% (oxazepam) and 64% (lorazepam).