- Transition-Metal-Free Synthesis of Acridones via Base-Mediated Intramolecular Oxidative C?H Amination
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Intramolecular oxidative C?H amination of 2-aminobenzophenones was achieved in the presence of potassium tert-butoxide and dimethyl sulfoxide. A series of functionalized acridones were prepared in moderate to excellent yields in a mild, efficient, and transition-metal-free manner. (Figure presented.).
- Wei, Wen-Tao,Sheng, Jian-Fei,Miao, Hui,Luo, Xiang,Song, Xian-Heng,Yan, Ming,Zou, Yong
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supporting information
p. 2101 - 2106
(2018/06/14)
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- Preparation process of lormetazepam impurity
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The invention belongs to the technical field of medicine synthesis and in particular relates to a preparation process of a lormetazepam impurity. The preparation process comprises the following steps: adding 2-amino-2',5-dichlorobenzophenone and potassium carbonate into a solvent; dropwise adding iodomethane and keeping heat and reacting; after reacting, carrying out post-treatment to obtain a lormetazepam impurity, wherein the post-treatment comprises the step of decompressing and evaporating to remove the solvent, adding purified water into restudies to dissolve residual salt, adding ethyl acetate to dissolve organic matters, separating out a water phase, concentrating an organic phase and crystallizing, and filtering to obtain the lormetazepam impurity. The solvent is THF (Tetrahydrofuran), DMF (Dimethyl Formamide) or DMSO (Dimethylsulfoxide). According to the preparation process, the 2-amino-2',5-dichlorobenzophenone is used as a raw material and the iodomethane is used as a methylation reagent; the target product impurity is obtained through one step of reaction, the conversion rate exceeds 98 percent and the yield exceeds 95 percent; a poisonous reagent is not used so that pollution to environment is reduced; meanwhile, less wastewater is reduced and the raw material is easy to obtain; compared with an existing process, the preparation process has great advantages.
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Paragraph 0027; 0028
(2017/07/22)
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- A Convenient Preparation of Alkylaminobenzophenones from 2,1-Benzisoxazolium Salts and Iodotrimethylsilane
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2-Alkylaminobenzophenones (2) have been prepared in good yields from 2,1-benzisoxazolium salts (1) and iodotrimethylsilane.
- Konwar, D.,Boruah, R. C.,Sandhu, J. S.
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p. 975 - 976
(2007/10/02)
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- Screening, detection and biotransformation of lormetazepam, a new hypnotic agent from the 1,4-benzodiazepine series
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The paper describes a screening procedure for 7-chloro-5-(2-chlorophenyl)-3-hydroxy-1-methyl-2,3-dihydro-1H-1,4-benzodiaze pin-2-one (lormetazepam, Noctamid) and other important analytical data (TLC, GLC, UV-, IR- and mass spectra) of this new benzodiazepine derivative. Screening results after a single p.o. dose of 1 mg lormetazepam (Noctamid-1) are also reported.
- Schutz,Fitz
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p. 177 - 183
(2007/10/02)
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- AN ALTERNATIVE SYNTHESIS OF DIPEPTIDO-AMINOBENZOPHENONE AND NOVEL HETEROCYCLIC FORMATIONS OF RING-OPENED 1,4-BENZODIAZEPINE DERIVATIVES
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An alternative synthesis of Gly-Gly-N-methylaminobenzophenone (1a) via iodoacetyl glycylaminobenzophenone (2) is described.Novel ring closures of 2 and cyano derivative 3 are also reported.
- Hirai, Kentaro,Ishiba, Teruyuki,Fujishita, Toshio,Sugimoto, Hirohiko
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p. 635 - 638
(2007/10/02)
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