59467-68-4Relevant academic research and scientific papers
Convergent syntheses of carbon-13 labeled midazolam and 1′-hydroxymidazolam
Zhang, Yinsheng,Woo, Peter W.K.,Hartman, Jon,Colbry, Norman,Huang, Yun,Huang, Che C.
, p. 2087 - 2091 (2005)
For the purpose of drug interaction studies, the stable-isotope labeled [13C3]midazolam and its metabolite, 1′-hydroxy- [13C3]midazolam were synthesized in four and five steps in overall yields of 25.5% and 14.2%, from 7-chloro-5-(2-fluorophenyl)-2-(N- nitrosomethylamino)-3H-1,4-benzodiazepine, respectively, by a convergent synthesis, in which a key imidazoline ring formation was achieved by the facile reaction of [13C]2-aminomethyl-7-chloro-2,3-dihydro-5-(2- fluorophenyl)-1H-1,4-benzodiazepine with varying ethyl imidate hydrochlorides. The scrambling of C-3 and C-4 labeling in intermediate diamine, and consequently in the final products, as well as the formation of a Δ4,5 isomer of 1′-hydroxy-[13C3]midazolam was observed and explained.
Benzophenone glycinamide derivatives
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, (2008/06/13)
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.
