- Benzodiazepines method for the preparation of compound
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The invention relates to a method for preparing benzodiazepine compounds, and discloses a method for preparing 8-R2-6-(2-R1-phenyl)-1-methyl-3a,4-dihydro-3H-imidazo[1,5-a][1,4] benzodiazepine (midbody II) and 8-R2-6-(2-R1-phenyl)-1-methyl-4H-imidazo[1,5-a][1,4] benzodiazepine (product III), wherein R is hydrogen, fluorine, chlorine, bromine or iodine; R2 is fluorine, chlorine, bromine or iodine. The midbody II is prepared from 7-R2-5-(2-R1-phenyl)-2-aminomethyl-2,3-dihydro-1H-[1,4] benzodiazepine and triethyl orthoacetate as raw materials through ultrasonic reaction; the product III is prepared by performing enzyme dehydrogenation on the midbody II. By adopting the technical scheme of the invention, the dehydrogenation reaction selectivity is improved, and the reaction yield is improved.
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Paragraph 0032; 0033; 0034; 0035
(2016/10/08)
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- PROCESS FOR PRODUCING HIGHLY PURE MIDAZOLAM AND SALTS THEREOF
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Provided is a process for producing highly pure midazolam and salts thereof, and a pharmaceutical composition containing the highly pure midazolam and/or a salt thereof.
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Page/Page column 5-6
(2009/04/24)
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- Imidazodiazepines and processes therefor
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Novel Imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included within the purview of the invention encompasses a compound of the formula STR1 wherein R1 is hydrogen and lower alkyl preferably methyl; R3 and R5 are hydrogen; R4 is hydrogen, nitro and halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof, R6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R2 is hydrogen and lower alkyl.
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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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