CAS No.5786-21-0,Clozapine Suppliers

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Basic Information

Molecular Structure:
CAS No.:	5786-21-0
Name:	Clozapine
Article Data:	19

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

Synthetic route

: clozapine N-oxide

: 5786-21-0
clozaril

Conditions

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

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

: clozapine N-oxide

: 4407-36-7
(2E)-3-phenyl-2-propen-1-ol

A: 63157-81-3
1-phenyl-propane-1,2,3-triol

B: 5786-21-0
clozaril

Conditions

Conditions	Yield
With osmium(VIII) oxide In water; tert-butyl alcohol at 20℃; for 19h; Inert atmosphere;	A 73% B 84%

...Expand

: 65514-72-9
N-(4-chloro-2-nitrophenyl)-N-{2-[(4-methylpiperazin-1-yl)carbonyl]phenyl}amine

: 5786-21-0
clozaril

Conditions

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

: N-{4-chloro-2-[(triphenylphosphoranylidene)amino]phenyl}-N-{2-[(4-methylpiperazin-1-yl)carbonyl]phenyl}amine

: 5786-21-0
clozaril

Conditions

Conditions	Yield
With triphenylphosphine at 230℃;	65%

: 292638-84-7
styrene

: clozapine N-oxide

A: 93-56-1
phenylethane 1,2-diol

B: 5786-21-0
clozaril

Conditions

Conditions	Yield
With osmium(VIII) oxide In water; tert-butyl alcohol at 20℃; for 19h; Inert atmosphere;	A 8% B 53%

...Expand

: 89-63-4
4-Chloro-2-nitroaniline

: 5786-21-0
clozaril

Conditions

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

: 108-86-1
bromobenzene

: 5786-21-0
clozaril

Conditions

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

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

: 118-91-2
ortho-chlorobenzoic acid

: 5786-21-0
clozaril

Conditions

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

Raw Materials

109-01-3

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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: Harmful Xn, Irritant 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.