cas 28911-01-5, Triazolam | Articles data

Articles about 28911-01-5Total 13 be found

IMPROVED PROCESS FOR PREPARATION OF TRIAZOL-BENZODIAZEPINE DERIVATIVES
An improved process for preparation of triazol-benzodiazepine derivatives, such as alprazolam, triazolam, brotizolam and etizolam, is presented. The process comprises a cyclization reaction of compound Formula B in toluene with catalytic amount of p-toluene sulphonic acid to obtain the triazol-benzodiazepine derivative of Formula C: wherein R is, and X is hydrogen or halogen.
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(2012/06/30)

PROCESS FOR PREPARATION OF TRIAZOL-BENZODIAZEPINE DERIVATIVES
An improved process for preparation of triazol-benzodiazepine derivatives, such as alprazolam, triazolam, brotizolam and etizolam, is presented. The process comprises a cyclization reaction of compound Formula B in toluene with catalytic amount of p-toluene sulphonic acid to obtain the triazol-benzodiazepine derivative of Formula C: wherein R is, and X is hydrogen or halogen.
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(2009/04/24)

1,4-Benzodiazepine N-nitrosoamidines: Useful intermediates in the synthesis of tricyclic benzodiazepines
1,4-Benzodiazepine N-nitrosoamidines have been used as scaffolds for the preparation of different tricyclic derivatives. Replacement of the N-nitrosoamidine moiety through treatment with the nucleophiles acetylhydrazine, aminoacetaldehyde dimethylacetal and 1-amino-2-propanol, followed by an acid-catalyzed cyclization step, afforded triazolo and imidazobenzodiazepines 1, 6, and 7, respectively, in good yields. When acetylhydrazine is used as a nucleophile, the overall process provides an alternative route to alprazolam (1b) and triazolam (1c), respectively.
Fustero, Santos,Gonzalez, Javier,Del Pozo, Carlos
p. 583 - 588
(2007/10/03)

Cyclodextrin complexes of benzodiazepines
Methods for enhancing the complexation efficiency of a drug with cyclodextrin and for enhancing the availability of a drug following administration of a cyclodextrin-drug complex.
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(2008/06/13)

Certain PAF antagonist/antihistamine combinations and methods
Methods and compositions are disclosed employing combinations of antihistamines with certain diaryl tetrahydrofuran, diaryl tetrahydrothiophene, triazolobenzodiazepine or thienotriazolodiazepine PAF--antagonist compounds in the treatment of allergic reactions.
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(2008/06/13)

Phosphorylation of cyclic amides
Compounds of the general formula STR1 are reacted with a strong base followed by a phosphorylating agent, such as dicyclicaminophosphinic halide or bis-di-lower alkylaminophosphinic halide to produce an imine of the formula STR2 wherein R is dicyclicaminophosphinyloxy or bis-di-lower alkylaminophosphinyloxy. R represents a leaving group which will undergo nucleophilic displacement with nitrogen, oxygen, sulfur and carbon containing nucleophiles, that is, nucleophiles which have, as a reactive site, a nitrogen, oxygen, sulfur or carbon atom, such that, when the cyclic imine undergoes nucleophilic displacement, there is formed C--N, C--O, C--S and C--C bonds between the carbon atom of the cyclic imine and the nucleophilic group. The end products may be utilized as intermediates in the production of pharmaceutically valuable compounds and, in some instances, are pharmaceutically valuable compounds per se.
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(2008/06/13)

S-substituted derivatives of 8-chloro-6-(2-chlorophenyl)-1-mercaptomethyl 4H-s-triazolo[4,3-a]-1,4-benzodiazepine; synthesis and pharmacology
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Vejdelek,Metys,Protiva
p. 123 - 136,123-136)
(2007/10/02)

Kinetics and mechanism of the equilibrium reaction of triazolam in aqueous solution
The equilibrium kinetics of triazolam in aqueous solution was investigated in the pH range of 1-11 at body temperature. The quantitative study indicated that it forms equilibrium mixtures consisting of ring-opened and closed forms with the composition being dependent on pH. The equilibrium constants of the two species in the pH range studied were determined by GLC method. The apparent first-order rate constants were estimated from the decreasing or increasing absorbance of the mixture in solutions. The forward-reaction rate constant (k(f)) showed a bell-shaped k(f)-pH profile with a rate maximum at pH 4.59, which indicates not only that the carbinolamine intermediate forms during equilibrium reaction, but that the rate-determining step of the reaction differs for the acidic and basic side of the rate maximum. The reverse-reaction rate constant decreased with increasing pH and could not be estimated in the pH region >5.65. Theoretical curves for both forward and reverse reactions satisfactorily fit the observed data. The pKa values of triazolam and its opened-form amine were estimated to be 1.52 and 6.50, respectively.
Konishi,Hirai,Mori
p. 1328 - 1334
(2007/10/02)

Novel synthesis of the pharmacologically important 1-substituted-6-phenyl-4H-s-triazolo[4,3-α][1,4]benzodiazepines
Several 6-phenyl-4H-s-triazolo[4,3-α][1,4]benzodiazepines have useful biological activity both in experimental animals and in man. This manuscript describes a novel synthesis of these compounds from intermediates that do not have a pre-formed benzodiazepine ring system.
Hester Jr.
p. 575 - 581
(2007/10/02)

2-[3-(Phthalimidomethyl)-5-methyl-4H-1,2,4-triazol-4-yl]benzophenones
A process to make 6-phenyl-4H-s-triazolo[4,3-a][1,4]-benzodiazepines by converting 2-[3-(hydroxymethyl)-4H-1,2,4-triazol-4-yl]benzophenones to 2-[3-[(phthalimido or methanesulfonyl)methyl]-4H-1,2,4-triazol-4-yl]benzophenones and converting these compounds to the highly active 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines useful as tranquilizers and sedatives.
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(2008/06/13)

6-Phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines
6-Phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula (IV): SPC1 wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, phenyl, benzyl and -COOR' in which R' is alkyl of 1 to 4 carbon atoms, inclusive; wherein R1 is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, inclusive; and wherein R2, R3, R4 and R5 are selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, halogen, nitro, cyano, trifluoromethyl, and alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoylamino and dialkylamino in which the carbon chain moieties are of 1 to 3 carbon atoms, inclusive, are produced by condensing a 1,3-dihydro-5-phenyl-2H-1,4-benzodiazepine-2-thione of the formula (I): SPC2 wherein R1, R2, R3, R4 and R5 are defined as above, with an organic acid hydrazide of the formula: EQU1 wherein R is defined as above. The new products of formula IV including their pharmacologically acceptable acid addition salts are useful as sedatives, tranquilizers and muscle relaxants in mammals and birds.
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(2008/06/13)

6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines which have central nervous system depressant activity.
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Hester Jr.,Rudzik,Kamdar
p. 1078 - 1081
(2007/10/05)