- Preparation method of 7-chloro-5-(2-fluorophenyl)-3H-1, 4-benzodiazepin-2-methylamine
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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.
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Paragraph 0043; 0045-0046; 0048-0049; 0051-0052; 0054
(2020/12/15)
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- 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine for forensic science, preparation method therefor and application of 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine
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The invention discloses 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine with a structure represented by a formula shown in the description. A preparation method for the8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine comprises the following steps: (1) synthesizing a compound B from a compound A; (2) synthesizing a compound C from the compound B; and (3) synthesizing the 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine compound D from the compound C. Shown by application researches on the 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine, the prepared 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine can be applied to reference materials for detection and identification work of organs of public security. The technical scheme of the invention achieves the following beneficial technical effects that an optimal synthesis route for synthesizing the 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine is optimized; the target object, i.e., the 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine is separated and purified, and thus, the purity of the 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine reaches 99% or more; and the prepared 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolbenzo[1,4]benzodiazepine can directly serve as a reference substance for the detection and identification work of the organs of public security.
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Paragraph 0074-0079
(2019/04/26)
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- Reactions of 1,4-benzodiazepinic N-nitrosoamidines with tosylmethyl isocyanide: A novel synthesis of midazolam
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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.
- Del Pozo, Carlos,Macias, Alberto,Alonso, Eduardo,Gonzalez, Javier
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p. 2697 - 2703
(2007/10/03)
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- Benzophenone glycinamide derivatives
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This invention is directed toward pharmacologically active compounds of the formula STR1 wherein A represents a nitrogen atom which may be substituted by a methyl, cyclopropylmethyl, di(C1-4 alkyl)aminoethyl, methoxymethyl or hydroxyethyl group and B represents a carbonyl group or A and B together represent a grouping of the formula STR2 in which Ra represents a hydrogen atom or a lower alkyl or hydroxymethyl group and X represents a nitrogen atom or C--Rb wherein Rb represents a hydrogen atom or a lower alkyl or hydroxymethyl group; R represents a halogen atom or a nitro or trifluoromethyl group; R1 represents a hydrogen atom or a lower alkyl group; R2 represents an acyl group derived from a naturally occurring amino acid (all such groups which contain an asymmetric carbon atom having the L- or D,L-configuration) and R3 represents a phenyl, halophenyl or 2-pyridyl group And acid addition salts thereof. Also provided are methods for their preparation and intermediates thereof. These compounds exhibit activity as anticonvulsants, muscle relaxants and sedatives.
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