14405-03-9Relevant articles and documents
Preparation method of lorazepam intermediate
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Paragraph 0068-0071; 0080-0083, (2020/12/15)
The invention provides a preparation method of a lorazepam intermediate, the lorazepam intermediate is 7-chloro-5-(2-chlorphenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-one-4-oxide, and the preparationmethod comprises the following steps: (1) carrying out acylation reaction on 2-amino-2', 5-dichlorobenzophenone and chloroacetyl chloride to prepare 2-chloroacetamido-2', 5-dichlorobenzophenone, (2) reacting 2-chloroacetamido-2', 5-dichlorobenzophenone with urotropine and ammonium acetate to prepare 7-chloro-5-(2-chlorphenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-one, and (3) carrying out a reaction on the 7-chloro-5-(2-chlorphenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-one and ammonium acetate to obtain 7-chloro-5-(2-chlorphenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-one-4-oxide. The preparationmethod disclosed by the invention is simple and convenient, mild in reaction condition, high in yield, good in product quality and low in cost.
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
Cheng, Pi,Zhang, Quan,Ma, Yun-Bao,Jiang, Zhi-Yong,Zhang, Xue-Mei,Zhang, Feng-Xue,Chen, Ji-Jun
supporting information; scheme or table, p. 3787 - 3789 (2009/04/06)
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).