Estazolam

Estazolam Basic information
Description Pharmacology Adverse reactions
Product Name:Estazolam
Synonyms:2,4)triazolo(4,3-a)(1,4)-benzodiazepine,8-chloro-6-phenyl-4h-(;3-a)(1,4)benzodiazepine,8-chloro-6-phenyl-4h-s-triazolo(;4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-6-phenyl-;4H-s-Triazolo(4,3-a)(1,4)benzodiazepine, 8-chloro-6-phenyl-;Julodin;Nemurel;Nuctalon;ProSom
CAS:29975-16-4
MF:C16H11ClN4
MW:294.74
EINECS:249-982-4
Product Categories:Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals
Mol File:29975-16-4.mol
Estazolam Structure
Estazolam Chemical Properties
Melting point 228-229°
Boiling point 448.04°C (rough estimate)
density 1.2294 (rough estimate)
refractive index 1.6110 (estimate)
Fp 11 °C
storage temp. 2-8°C
solubility DMF: 30 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 20 mg/ml; Ethanol: 10 mg/ml
pkapKa 2.84(H2O) (Uncertain)
form A crystalline solid
CAS DataBase Reference29975-16-4(CAS DataBase Reference)
IARC3 (Vol. 66) 1996
NIST Chemistry ReferenceEstazolam(29975-16-4)
Safety Information
Hazard Codes Xi,T,F
Risk Statements 36/37/38-39/23/24/25-23/24/25-11
Safety Statements 36/37/39-45-36/37-16-7
RIDADR 3249
WGK Germany 3
RTECS XZ5473500
HazardClass 6.1(b)
PackingGroup III
HS Code 2933910000
ToxicityLD50 orally in male mice, rats and rabbits: 740, 3200, 300 mg/kg (Yokotani)
MSDS Information
Estazolam Usage And Synthesis
DescriptionEstazolam, sold under the brand name Prosom among others, is a tranquilizer medication of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring . It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. 
PharmacologyEstazolam is classed as a "triazolo" benzodiazepine drug.Estazolam exerts its therapeutic effects via its benzodiazepines receptor agonist properties.Estazolam at high doses decreases histamine turnover via its action at the benzodiazepine-GABA receptor complex in mouse brains.
Adverse reactionsCommon adverse reactions such as drowsiness, drowsiness, dizziness, fatigue, unsteady gait, etc., increasing the dose may occasionally cause adverse reactions such as headache, ataxia, motor dysfunction, slurred speech, respiratory depression, tremor, etc. Long-term use can lead to memory loss Adverse reactions such as decline, weight gain, cognitive impairment, loss of libido, etc. In addition, long-term use of estazolam can cause down-regulation of benzodiazepine receptors in the central nervous system, which can lead to tolerance and dependence, and sudden withdrawal can cause Headache, insomnia, depression, nervousness, restlessness, irritability, anxiety, tremor, tachycardia and other withdrawal symptoms, namely drug addiction, are the most serious adverse reactions of long-term use of estazolam.
OriginatorEurodin,Takeda,Japan,1975
UsesA benzodiazepine derivative possessing anxiolytic, anticonvulsant, and muscle relaxant properties. It is commonly prescribed to treat short-term insomnia. Controlled Substance.
DefinitionChEBI: A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term ma agement of insomnia.
Manufacturing ProcessA mixture of 5.74 grams (0.020 mol) of 7-chloro-1,3-dihydro-5-phenyl-2H- 1,4-benzodiazepine-2-thione, 3.6 grams (0.060 mol) of formic acid hydrazide and 200 ml of 1-butanol was refluxed for 3.75 hours with a slow stream of nitrogen bubbling through the mixture. The mixture was concentrated, the residue was suspended in water and the suspension was filtered. The filter cake consisted principally of unchanged starting material. The filtrate was concentrated, ethyl acetate and Skellysolve B hexanes being added during the concentration, giving crude product (2.54 grams), MP 220.5° to 225°C. Recrystallization of this material from ethyl acetate-Skellysolve B hexanes gave 8-chloro-6-phenyl-4H-s-triazolo[4,3-a] [1,4]benzodiazepine, MP 228° to 229°C.
Brand nameProsom (Abbott).
Therapeutic FunctionHypnotic, Sedative
Chlorodimethylphenylsilane Ribavirin ESTAZOLAM-D5 ALPHA-HYDROXYTRIAZOLAM Chloroacetic acid U46,195 ALPHA-HYDROXYALPRAZOLAM-D5 1H-Benzotriazole ALPRAZOLAM-D5 Difluorochloromethane ADINAZOLAM PHENYL VALERATE Benzodiazepine CHLOROPHENYLSILANE 97 Phenylhydrazine Estazolam tert-Butylchlorodiphenylsilane 4-HYDROXYALPRAZOLAM

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