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| CAS No.: | 5786-21-0 |
|---|---|
| Name: | Clozapine |
| Molecular Structure: | |
|
|
|
| Formula: | C18H19ClN4 |
| Molecular Weight: | 326.829 |
| Synonyms: | Clorazil;Fazaclo;Iprox;Clozapina [INN-Spanish];8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine;5H-Dibenzo(b,e)(1,4)diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)-;Leponex;Asaleptin;Clozaril (TN);Clozapine [USAN:BAN:INN];8-chloro-11（4-methy-1-piperaziong）-5-H-dibenzo[b,e][1.4]diazepine; |
| EINECS: | 227-313-7 |
| Density: | 1.319 g/cm3 |
| Melting Point: | 182-185 °C |
| Boiling Point: | 489.159 °C at 760 mmHg |
| Flash Point: | 249.635 °C |
| Solubility: | ethanol: 1 mg/mL |
| Appearance: | Yellow Crystalline Solid |
| Hazard Symbols: |
 Xn,  Xi
|
| Risk Codes: | 22-36/37/38 |
| Safety: | 26 |
| Transport Information: | UN 2811 6.1/PG 3 |
| PSA: | 30.87000 |
| LogP: | 3.17210 |
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- 5786-21-0
clozaril
| Conditions | Yield |
|---|---|
| With hydrogenchloride; titanium(III) chloride In water; acetonitrile at 20℃; for 1h; | 97% |
- 109-01-3
1-methyl-piperazine
- 50892-62-1
8-chloro-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one
- 5786-21-0
clozaril
| Conditions | Yield |
|---|---|
| With titanium tetrachloride In 1,4-dioxane; toluene for 2h; Heating; | 88% |
| With titanium tetrachloride | 53% |
| With hydrogenchloride; titanium tetrachloride In water; methoxybenzene; isopropyl alcohol; toluene | |
| With titanium tetrachloride |
| Conditions | Yield |
|---|---|
| With osmium(VIII) oxide In water; tert-butyl alcohol at 20℃; for 19h; Inert atmosphere; | A 73% B 84% |
- 65514-72-9
N-(4-chloro-2-nitrophenyl)-N-{2-[(4-methylpiperazin-1-yl)carbonyl]phenyl}amine
- 5786-21-0
clozaril
| Conditions | Yield |
|---|---|
| With tributylphosphine at 150℃; for 48h; Temperature; Reagent/catalyst; | 80% |
| Multi-step reaction with 2 steps 1: 3 h / 150 °C 2: triphenylphosphine / 230 °C View Scheme |
- 5786-21-0
clozaril
| Conditions | Yield |
|---|---|
| With triphenylphosphine at 230℃; | 65% |
| Conditions | Yield |
|---|---|
| With osmium(VIII) oxide In water; tert-butyl alcohol at 20℃; for 19h; Inert atmosphere; | A 8% B 53% |
| Conditions | Yield |
|---|---|
| Multi-step reaction with 5 steps 1.1: o-xylene / Dean-Stark 1.2: Reflux 2.1: iron; calcium chloride / water / 90 - 100 °C 3.1: triethylamine / dichloromethane / 0.33 h / 20 °C 3.2: 2.33 h / 20 °C 4.1: titanium tetrachloride / o-xylene / 10 - 15 °C / Reflux 5.1: titanium tetrachloride / 10 °C / Reflux View Scheme | |
| Multi-step reaction with 6 steps 1.2: 12 h / 20 °C / Reflux 2.1: iodine / 3 h / 50 - 55 °C 3.1: sodium dithionate / methanol / 2 h / 50 - 55 °C 4.1: toluene / 0 - 5 °C 5.1: trichlorophosphate / 3 h / Reflux 6.1: potassium carbonate / ethanol / 3 h / Reflux View Scheme |
| Conditions | Yield |
|---|---|
| Multi-step reaction with 6 steps 1.2: 12 h / 20 °C / Reflux 2.1: iodine / 3 h / 50 - 55 °C 3.1: sodium dithionate / methanol / 2 h / 50 - 55 °C 4.1: toluene / 0 - 5 °C 5.1: trichlorophosphate / 3 h / Reflux 6.1: potassium carbonate / ethanol / 3 h / Reflux View Scheme |
- 16611-15-7
N-(4-chloro-2-nitrophenyl)benzenamine
- 5786-21-0
clozaril
| Conditions | Yield |
|---|---|
| Multi-step reaction with 5 steps 1: iodine / 3 h / 50 - 55 °C 2: sodium dithionate / methanol / 2 h / 50 - 55 °C 3: toluene / 0 - 5 °C 4: trichlorophosphate / 3 h / Reflux 5: potassium carbonate / ethanol / 3 h / Reflux View Scheme |
| Conditions | Yield |
|---|---|
| Multi-step reaction with 5 steps 1.1: o-xylene / Dean-Stark 1.2: Reflux 2.1: iron; calcium chloride / water / 90 - 100 °C 3.1: triethylamine / dichloromethane / 0.33 h / 20 °C 3.2: 2.33 h / 20 °C 4.1: titanium tetrachloride / o-xylene / 10 - 15 °C / Reflux 5.1: titanium tetrachloride / 10 °C / Reflux View Scheme |
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Chemistry
Empirical Formula: C18H19ClN4
Molecular Weight: 326.8233 g/mol
EINECS: 227-313-7
Index of Refraction: 1.681
Density: 1.31 g/cm3
Flash Point: 249.6 °C
Melting point: 182-185 °C
Solubility: Ethanol: 1 mg/mL
Appearance: Yellow crystalline solid
Enthalpy of Vaporization: 75.54 kJ/mol
Boiling Point: 489.2 °C at 760 mmHg
Vapour Pressure: 1.02E-09 mmHg at 25 °C
Structure of Clozapine (CAS NO.5786-21-0):
IUPAC Name: 3-Chloro-6-(4-methylpiperazin-1-yl)-5H-benzo[c][1,5]benzodiazepine
Product Category: Active Pharmaceutical Ingredients;Intermediates & Fine Chemicals;Dopamine receptor
History
Clozapine (CAS NO.5786-21-0) by Sandoz in 1961, and introduced in Europe in 10 years. In 1975, the report of agranulocytosis leading to death in some patients treated with clozapine, clozapine manufacturers to voluntarily withdraw. Clozapine fell out of favor for more than a decade. However, studies have shown that clozapine is more effective for refractory schizophrenia than other antipsychotics, the U.S. Food and Drug Administration and health authorities in most other countries approved its use only for refractory schizophrenia Patients require regular blood tests to monitor the neutrophil, and then agranuloctytosis development. December 2002, clozapine was also approved to reduce the risk of suicide in patients with schizophrenia or schizoaffective is considered in the risk of suicide.
Uses
Clozapine (CAS NO.5786-21-0) can be used as an antipsychotic.
Production
Clozapine (CAS NO.5786-21-0) can be obtained from the reaction of 2 - Amino -4 - chloro-aniline 2 -2 '- carboxylic acid (4''-methyl) piperazine with Phosphorus oxychloride .
Toxicity Data With Reference
| Organism | Test Type | Route | Reported Dose (Normalized Dose) | Effect | Source |
|---|---|---|---|---|---|
| child | TDLo | oral | 4762ug/kg (4.762mg/kg) | BEHAVIORAL: ATAXIA BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY) BEHAVIORAL: ANTIPSYCHOTIC | American Journal of Emergency Medicine. Vol. 14, Pg. 462, 1996. |
| dog | LD50 | oral | 145mg/kg (145mg/kg) | GASTROINTESTINAL: NAUSEA OR VOMITING | Farmaco, Edizione Pratica. Vol. 26, Pg. 585, 1971. |
| guinea pig | LD50 | oral | 510mg/kg (510mg/kg) | Farmaco, Edizione Pratica. Vol. 26, Pg. 585, 1971. | |
| human | TDLo | oral | 5mg/kg/7D-I (5mg/kg) | CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP | Arzneimittel-Forschung. Drug Research. Vol. 22, Pg. 919, 1972. |
| man | TDLo | oral | 4286ug/kg/11D (4.286mg/kg) | GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA" BLOOD: CHANGES IN CELL COUNT (UNSPECIFIED) | Journal of Clinical Pyschopharmacology. Vol. 13, Pg. 155, 1993. |
| man | TDLo | oral | 5357ug/kg/5D- (5.357mg/kg) | BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS" BEHAVIORAL: ANTIPSYCHOTIC CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP | Journal of Clinical Pyschopharmacology. Vol. 12, Pg. 139, 1992. |
| man | TDLo | oral | 27mg/kg/13D-I (27mg/kg) | AUTONOMIC NERVOUS SYSTEM: "SMOOTH MUSCLE RELAXANT (MECHANISM UNDEFINED, SPASMOLYTIC)" BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS" BEHAVIORAL: ATAXIA | Journal of Clinical Psychiatry. Vol. 55, Pg. 38, 1994. |
| man | TDLo | oral | 40mg/kg (40mg/kg) | BEHAVIORAL: COMA LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION VASCULAR: BP LOWERING NOT CHARACTERIZED IN AUTONOMIC SECTION | Veterinary and Human Toxicology. Vol. 41, Pg. 20, 1999. |
| man | TDLo | oral | 86mg/kg/15D-I (86mg/kg) | CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES | British Journal of Psychiatry. Vol. 173, Pg. 440, 1998. |
| man | TDLo | oral | 270mg/kg/6W-I (270mg/kg) | LUNGS, THORAX, OR RESPIRATION: STRUCTURAL OR FUNCTIONAL CHANGE IN TRACHEA OR BRONCHI BLOOD: AGRANULOCYTOSIS GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA" | Annales de Medecine Interne. Vol. 144, Pg. 494, 1993. |
| man | TDLo | oral | 429mg/kg/60D- (429mg/kg) | BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY) | American Journal of Psychiatry. Vol. 152, Pg. 649, 1995. |
| man | TDLo | oral | 429mg/kg (429mg/kg) | BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY) CARDIAC: PULSE RATE INCREASE WITHOUT FALL IN BP BEHAVIORAL: COMA | Journal of Toxicology, Clinical Toxicology. Vol. 38, Pg. 325, 2000. |
| man | TDLo | oral | 2211mg/kg/37W (2211mg/kg) | BLOOD: "CHANGES IN SERUM COMPOSITION (E.G., TP, BILIRUBIN, CHOLESTEROL)" | Journal of Clinical Pyschopharmacology. Vol. 15, Pg. 287, 1995. |
| man | TDLo | oral | 3280mg/kg/82W (3280mg/kg) | BLOOD: AGRANULOCYTOSIS | American Journal of Psychiatry. Vol. 153, Pg. 1503, 1996. |
| mouse | LD50 | intraperitoneal | 90mg/kg (90mg/kg) | BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY) LUNGS, THORAX, OR RESPIRATION: DYSPNEA | Farmaco, Edizione Pratica. Vol. 26, Pg. 585, 1971. |
| mouse | LD50 | intravenous | 36500ug/kg (36.5mg/kg) | BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD | Kiso to Rinsho. Clinical Report. Vol. 7, Pg. 667, 1973. |
| mouse | LD50 | oral | 150mg/kg (150mg/kg) | Journal of Medicinal Chemistry. Vol. 23, Pg. 878, 1980. | |
| mouse | LD50 | subcutaneous | 194mg/kg (194mg/kg) | BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) BEHAVIORAL: EXCITEMENT BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD | Kiso to Rinsho. Clinical Report. Vol. 7, Pg. 667, 1973. |
| rat | LD50 | intramuscular | 210mg/kg (210mg/kg) | Farmaco, Edizione Pratica. Vol. 26, Pg. 585, 1971. | |
| rat | LD50 | intravenous | 41600ug/kg (41.6mg/kg) | BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION BEHAVIORAL: ATAXIA | Kiso to Rinsho. Clinical Report. Vol. 7, Pg. 667, 1973. |
| rat | LD50 | oral | 251mg/kg (251mg/kg) | Kiso to Rinsho. Clinical Report. Vol. 7, Pg. 667, 1973. | |
| rat | LD50 | subcutaneous | 240mg/kg (240mg/kg) | BEHAVIORAL: ALTERED SLEEP TIME (INCLUDING CHANGE IN RIGHTING REFLEX) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION | Kiso to Rinsho. Clinical Report. Vol. 7, Pg. 667, 1973. |
| women | TDLo | oral | 20mg/kg (20mg/kg) | BEHAVIORAL: COMA BLOOD: LEUKOPENIA GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF ENDOCRINE PANCREAS | Annals of Internal Medicine. Vol. 121, Pg. 722, 1994. |
| women | TDLo | oral | 28mg/kg/2W-I (28mg/kg) | GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF ENDOCRINE PANCREAS | Lancet. Vol. 340, Pg. 251, 1992. |
| women | TDLo | oral | 96mg/kg/48D-I (96mg/kg) | BLOOD: LEUKOPENIA BLOOD: AGRANULOCYTOSIS | Human Psychopharmacology. Vol. 13, Pg. 583, 1998. |
| women | TDLo | oral | 104mg/kg/26D- (104mg/kg) | BLOOD: EOSINOPHILIA | Journal of Clinical Psychiatry. Vol. 59, Pg. 195, 1998. |
| women | TDLo | oral | 168mg/kg/4W-I (168mg/kg) | BLOOD: AGRANULOCYTOSIS | Netherlands Journal of Medicine. Vol. 52, Pg. 26, 1998. |
| women | TDLo | oral | 280mg/kg/5W-I (280mg/kg) | LIVER: "HEPATITIS (HEPATOCELLULAR NECROSIS), DIFFUSE" BLOOD: EOSINOPHILIA | American Journal of Psychiatry. Vol. 150, Pg. 985, 1993. |
Safety Profile
Hazard Codes: 
Xn,
Xi
Risk Statements: 22-36/37/38
R22:Harmful if swallowed.
R36/37/38:Irritating to eyes, respiratory system and skin.
Safety Statements: 26
S26: In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
Specification
Clozapine , its cas register number is 5786-21-0. It also can be called 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine ; Leponex ; and 5H-Dibenzo(b,e)(1,4)diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)- . Many minor though some serious and potentially fatal: the more common include constipation, drooling, muscle stiffness, sedation, tremors, orthostasis, hyperglycemia, and weight gain. Extrapyramidal symptoms may subside somewhat after a person switches from another antipsychotic to Clozapine. Clozapine (CAS NO.5786-21-0) also carries black box warnings for seizures, myocarditis, and "other adverse cardiovascular and respiratory effects." Slow titration of dosing may also decrease the risk for orthostatic hypotension and other adverse cardiovascular side effects. It may have a synergistic effect with the sedating action of other drugs such as benzodiazepines, and thus respiratory depression may result with concomitant use. Care should be taken, especially if the latter drugs are given parenterally.