59467-61-7Relevant articles and documents
Preparation method of 7-chloro-5-(2-fluorophenyl)-3H-1, 4-benzodiazepin-2-methylamine
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Paragraph 0043; 0045-0046; 0048-0049; 0051-0052; 0054, (2020/12/15)
The invention provides a preparation method of 7-chloro-5-(2-fluorophenyl)-3H-1, 4-benzodiazepin-2-methylamine, which comprises the following steps: (1) reacting 7-chloro-5-(2-fluorophenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-one with phosphorus pentasulfide to obtain 7-chloro-5-(2-fluorophenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-thione, and (2) enabling the 7-chloro-5-(2-fluorophenyl)-1, 3-dihydro-2H-1, 4-benzodiazepin-2-thione to react with a methylamine alcohol solution, so as to prepare the 7-chloro-5-(2-fluorophenyl)-3H-1, 4-benzodiazepin-2-methylamine. The preparation method providedby the invention is low in cost, mild in condition, safe in production, high in yield, stable and reliable in product quality, simple and convenient to operate and more suitable for industrial production.
Reactions of 1,4-benzodiazepinic N-nitrosoamidines with tosylmethyl isocyanide: A novel synthesis of midazolam
Del Pozo, Carlos,Macias, Alberto,Alonso, Eduardo,Gonzalez, Javier
, p. 2697 - 2703 (2007/10/03)
Reaction of 1,4-benzodiazepinic N-nitrosoamidines, used as synthetic equivalents of imidoyl chlorides, with the monoanion of tosylmethyl isocyanide is described. The process gives entry to 3-(4-tosyl)imidazo[1,5-a][1,4] benzodiazepines, compounds which have not been described yet in the literature. These systems can be derivatized to the corresponding trisubstituted 1,4-benzodiazepines by alkylation or acylation of the imidazole ring. These new heterocyclic derivatives are potentially useful in the field of medicinal chemistry. In addition, midazolam 3, the anesthetic properties of which are well established, can be easily prepared in one step by desulfonylation of compound 7a.