Acyclovir supplier | CasNO.59277-89-3

Name
Acyclovir
EINECS 261-685-1
CAS No. 59277-89-3
Article Data50
CAS DataBase
Density 1.77 g/cm³
Solubility Water: 0.7 mg/mL
Melting Point 256-257 °C
Formula C₈H₁₁N₅O₃
Boiling Point 595 °C at 760 mmHg
Molecular Weight 225.207
Flash Point 313.6 °C
Transport Information
Appearance White to light yellow crystal powder
Safety 22-24/25-36-26
Risk Codes 36/37/38
Molecular Structure
Hazard Symbols Xi
Synonyms Acyclovir
PSA 119.05000
LogP -0.75060

Synthetic route

: 75128-73-3
2-acetylamino-9-(2-acetoxyethoxymethyl)purine-6-one

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With sodium hydroxide In water at 85 - 95℃; for 3h;	97.5%
With methylamine In water at 23℃; for 1h;	93%
With sodium hydroxide	92%

: 131490-71-6
1-<(2-hydroxyethoxy)methyl>-5-<(thiocarbamoyl)amino>-1H-imidazole-4-carboxamide

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With sodium hydroxide; copper diacetate for 1h; Heating;	92%
With sodium hydroxide; copper(II) ion at 100℃; for 1h; Product distribution; further metal ions and reaction conditions investigatet; reaction also with H2O2 / Na2WO4;	92%

: 112233-78-0
9-<(2-acetoxyethoxy)methyl>-2-N-acetyl-6-O-(diphenylcarbamoyl)guanine

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With ammonia In methanol; water at 60℃;	91%
With ammonium hydroxide In methanol at 60℃; for 24h;	91%

: 1336-21-6
ammonium hydroxide

: 75128-73-3
2-acetylamino-9-(2-acetoxyethoxymethyl)purine-6-one

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
In methanol	90%

: 81777-49-3
2-amino-6-chloro-9-<(2-hydroxyethoxy)methyl>-9H-purine

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With phosphoric acid; adenosine deaminase Ambient temperature; pH=7.5;	89%

: 59277-86-0
2,6-diamino-9-{(2-hydroxyethoxy)methyl}purine

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With phosphoric acid; adenosine deaminase Ambient temperature; pH=7.5;	89%

: 364634-35-5
9-(2-trimethylsilyloxyethoxymethyl)guanine

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With acetic acid In water at 80℃; for 2h;	85%

: 9-<(2-acetoxyethoxy)methyl>-2-N-phenylacetylguanine

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With ammonium hydroxide In methanol for 24h; Ambient temperature;	84%

: 127218-19-3
Acetic acid 2-(2-bromo-6-oxo-1,6-dihydro-purin-9-ylmethoxy)-ethyl ester

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With ammonia In methanol at 120℃;	80%

: 1400637-35-5
2-[(2-amino-6-oxo-3,6-dihydro-9H-purin-9-yl)methoxy]ethyl pyrrolidinophosphate ammonium salt

A: 59277-89-3
acycloguanosine

B: acyclovir monophosphate

Conditions

Conditions	Yield
With potassium chloride; potassium hydroxide In water at 25℃; pH=12;	A 80% B n/a

: 1400637-36-6
2-[(2-amino-6-oxo-3,6-dihydro-9H-purin-9-yl)methoxy]ethyl morpholinophosphate ammonium salt

A: 59277-89-3
acycloguanosine

B: acyclovir monophosphate

Conditions

Conditions	Yield
With potassium chloride; potassium hydroxide In water at 25℃; for 120h; pH=12;	A 80% B n/a

: 1400637-37-7
N-(2-morpholinoethyl)-2-[(2-amino-6-oxo-3,6-dihydro-9H-purin-9-yl)methoxy]ethyl phosphoramidate ammonium salt

A: 59277-89-3
acycloguanosine

B: acyclovir monophosphate

Conditions

Conditions	Yield
With potassium chloride; potassium hydroxide In water at 25℃; pH=12;	A 80% B n/a

: N,N-dipropyl-2-[(2-amino-6-oxo-3,6-dihydro-9H-purin-9-yl)methoxy]ethyl phosphoramidate ammonium salt

A: 59277-89-3
acycloguanosine

B: acyclovir monophosphate

Conditions

Conditions	Yield
With potassium chloride; potassium hydroxide In water at 25℃; pH=12;	A 80% B n/a

: 1400637-39-9
9-(2-hydroxyethoxymethyl)guanine phosphoromono-N,N-dimethylaminoethylamidate

A: 59277-89-3
acycloguanosine

B: acyclovir monophosphate

Conditions

Conditions	Yield
With potassium chloride; potassium hydroxide In water at 25℃; pH=12;	A 80% B n/a

: 1400637-40-2
9-(2-hydroxyethoxymethyl)guanine phosphoromono-3-dimethylamino-1-propylamidate

A: 59277-89-3
acycloguanosine

B: acyclovir monophosphate

Conditions

Conditions	Yield
With potassium chloride; potassium hydroxide In water at 25℃; pH=12;	A 80% B n/a

: 1400637-42-4
N-hexyl-2-[(2-amino-6-oxo-3,6-dihydro-9H-purin-9-yl)methoxy]ethyl phosphoramidate ammonium salt

A: 59277-89-3
acycloguanosine

B: acyclovir monophosphate

Conditions

Conditions	Yield
With potassium chloride; potassium hydroxide In water at 25℃; pH=12;	A 80% B n/a

: 646-06-0
1,3-DIOXOLANE

: 73-40-5
2-amino-1,9-dihydro-6H-purin-6-one

: 7440-44-0
pyrographite

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With trimethylsilyl trifluoromethanesulfonate; acetic acid; 1,1,1,3,3,3-hexamethyl-disilazane	78%
With trifluorormethanesulfonic acid; 1,1,1,3,3,3-hexamethyl-disilazane In water; acetic acid	73%
With ammonium hydroxide; sodium hydroxide; trifluorormethanesulfonic acid; acetic acid; 1,1,1,3,3,3-hexamethyl-disilazane In water; toluene	72%
With trifluorormethanesulfonic acid; acetic acid; 1,1,1,3,3,3-hexamethyl-disilazane In methanol; water	66.6%

...Expand

: 9-(benzoyloxyethoxymethyl)guanine

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With ammonia In methanol	75%

: 9-(2-trimethylsilylethoxymethyl)guanine

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With acetic acid In water	69%

: 661465-32-3
acyclovir P-(O-isopropyl) hydrogenphosphonate

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With human blood serum In water at 37℃; for 72h; Product distribution; Further Variations:; Reagents;	52%

: 59277-92-8
1-(2-amino-6-chloro-purin-9-ylmethoxy)-2-benzoyloxy-ethane

: 60-24-2
2-hydroxyethanethiol

A: 59277-89-3
acycloguanosine

B 9-(2-hydroxymethoxymethyl)guanine: 9-(2-hydroxymethoxymethyl)guanine

Conditions

Conditions	Yield
In methanol; methanolic sodium methylate; water	A n/a B 45%

...Expand

: 75128-77-7
9-<(2-hydroxyethoxy)methyl>-2-(methylthio)hypoxanthine

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With ammonia In ethanol at 140℃; for 60h;	39%
In ethanol; ammonia	15 mg (39%)

: 157722-20-8
acyclovir hydrogenphosphonate

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With human blood serum In water at 37℃; for 72h; Product distribution; Further Variations:; Reagents;	18%

: 59278-00-1
2-acetoxyethyl acetoxymethyl ether

: 108-24-7
acetic anhydride

: 118-00-3
G

A: 59277-89-3
acycloguanosine

B: 91702-61-3
7-(2-Hydroxyethoxymethyl)guanine

Conditions

Conditions	Yield
With sodium hydroxide; toluene-4-sulfonic acid 1.) 100 deg C, 20 h, 2.) room temperature, overnight; Yield given. Multistep reaction;	A n/a B 0.5%

...Expand

: 58305-05-8
(2-benzoyloxyethyl)oxymethyl chloride

: 73-40-5
2-amino-1,9-dihydro-6H-purin-6-one

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With ammonium sulfate; tetrabutyl ammonium fluoride 1.) hexamethyldisilazane, reflux, 24 h; 2.) THF/benzene, reflux, 3 h; Yield given. Multistep reaction;

: 73-40-5
2-amino-1,9-dihydro-6H-purin-6-one

: 1462-33-5
2-chloroethyl chloromethyl ether

A: 59277-89-3
acycloguanosine

B: 127302-85-6
9-<<2-chloroethoxy>methyl>guanine

Conditions

Conditions	Yield
With ammonium sulfate; tetrabutyl ammonium fluoride 1.) hexamethyldisilazane, reflux, 24 h; 2.) THF/benzene, reflux, 3 h; Yield given. Multistep reaction. Yields of byproduct given;
With ammonium sulfate; tetrabutyl ammonium fluoride 1.) hexamethyldisilazane, reflux, 24 h; 2.) THF/benzene, reflux, 4 h; Yield given. Multistep reaction. Yields of byproduct given;

...Expand

: 73-40-5
2-amino-1,9-dihydro-6H-purin-6-one

: 1462-35-7
1-bromo-2-(chloromethoxy)ethane

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With ammonium sulfate; tetrabutyl ammonium fluoride 1.) hexamethyldisilazane, reflux, 24 h; 2.) THF/benzene, reflux, 3 h; Yield given. Multistep reaction;

: 102728-64-3
9-[(acetoxyethoxy)methyl]guanine

: 59277-89-3
acycloguanosine

Conditions

Conditions	Yield
With methylamine at 80℃; for 0.5h;
With Dulbecco's Modified Phosphite-Buffer Saline; SIRC cell lysate at 34℃; pH=7.4; Kinetics; Further Variations:; Reagents;

: 59277-89-3
acycloguanosine

: 108-24-7
acetic anhydride

: 110104-37-5
2-acetylamino-9-<(2-hydroxyethoxy)methyl>-1,9-dihydro-6H-purin-6-one

Conditions

Conditions	Yield
With dmap for 120h; Ambient temperature;	98%

: 59277-89-3
acycloguanosine

: 4637-24-5
N,N-dimethyl-formamide dimethyl acetal

: N'-[9-(2-hydroxy-ethoxymethyl)-6-oxo-6,9-dihydro-1H-purin-2-yl]-N,N-dimethyl-formamidine

Conditions

Conditions	Yield
With N,N-dimethyl-formamide Condensation;	98%

: 59277-89-3
acycloguanosine

[poly(ethylene glycol)](NHCH2CH2COOH)2, MW: 1500 D: [poly(ethylene glycol)](NHCH2CH2COOH)2, MW: 1500 D

[poly(ethylene glycol)](NH-CH2CH2COO-aciclovir)2: [poly(ethylene glycol)](NH-CH2CH2COO-aciclovir)2

Conditions

Conditions	Yield
With dmap; triethylamine; bromo-tris(1-pyrrolidinyl)phosphonium hexafluorophosphate In N,N-dimethyl-formamide at 20℃; for 72h;	98%

: 59277-89-3
acycloguanosine

: 1036914-97-2
2-(2,2-dimethyl-3-trityloxypropanoyl)sulfanylethoxyphosphinic acid

: 1037071-44-5
9-(2-hydroxy-ethoxymethyl)-guanin-5'-yl-0-(triphenylmethyloxy-tert-butyl-5-acyl-2-thioethyl) H-phosphonate

Conditions

Conditions	Yield
With pivaloyl chloride In pyridine at -15 - 20℃; for 2h;	98%

: 59277-89-3
acycloguanosine

: 2082-76-0
capric anhydride

: 1360928-42-2
2-amino-9-[(2-decanoyloxy)ethyl-oxy-methyl]-1,9-dihydro-6H-purin-6-one

Conditions

Conditions	Yield
With dmap In dimethyl sulfoxide for 0.166667h; Inert atmosphere;	98%

: 59277-89-3
acycloguanosine

: 626-29-9
myristic anhydride

: 866215-87-4
2-amino-9-[(2-tetradecanoyloxy)ethyloxy-methyl]-1,9-dihydro-6H-purin-6-one

Conditions

Conditions	Yield
With dmap In dimethyl sulfoxide for 0.166667h; Inert atmosphere;	98%

: 59277-89-3
acycloguanosine

: 18162-48-6
tert-butyldimethylsilyl chloride

: 9-<<2-<(tert-butyl)dimethylsiloxy>ethoxy>methyl>guanidine

Conditions

Conditions	Yield
With 1H-imidazole at 25℃; for 48h;	97%

: 59277-89-3
acycloguanosine

: 18162-48-6
tert-butyldimethylsilyl chloride

: 139767-68-3
2-amino-9-[2-(tert-butyldimethylsilyloxy)ethoxymethyl]-1,9-dihydropurin-6-one

Conditions

Conditions	Yield
With 1H-imidazole In N,N-dimethyl-formamide at 20℃; for 48h;	97%
With 1H-imidazole In N,N-dimethyl-formamide at 20℃;	87%
With 1H-imidazole In N,N-dimethyl-formamide at 23℃; for 5h;	79%

: 59277-89-3
acycloguanosine

: 4637-24-5
N,N-dimethyl-formamide dimethyl acetal

: 100699-59-0
N'-(9-((2-hydroxyethoxy)-methyl)-6-oxo-6,9-dihydro-1H-purin-2-yl)-N,N-dimethylformimidamide

Conditions

Conditions	Yield
In N,N-dimethyl-formamide at 20℃; for 24h;	97%
In N,N-dimethyl-formamide at 20℃;

: 59277-89-3
acycloguanosine

: 2051-49-2
n-hexanoic anhydride

: 2-amino-9-[(2-hexanoyloxy)ethyl-oxy-methyl]-1,9-dihydro-6H-purin-6-one

Conditions

Conditions	Yield
With dmap In dimethyl sulfoxide for 0.166667h; Inert atmosphere;	97%
dmap In N,N-dimethyldecanoamide at 25℃; for 48h; Product distribution / selectivity; Inert atmosphere;	90%

: 59277-89-3
acycloguanosine

: 645-66-9
lauric anhydride

: 140900-50-1
2-amino-9-[(2-dodecanoyloxy)ethyl-oxymethyl]-1,9-dihydro-6H-purin-6-one

Conditions

Conditions	Yield
With dmap In dimethyl sulfoxide for 0.166667h; Inert atmosphere;	97%

: 106-31-0
butanoic acid anhydride

: 59277-89-3
acycloguanosine

: 64843-83-0
2-amino-9-[(2-butanoyloxy)ethyl-oxy-methyl]-1,9-dihydro-6H-purin-6-one

Conditions

Conditions	Yield
With dmap In dimethyl sulfoxide for 0.166667h; Inert atmosphere;	96%
With pyridine; dmap In N,N-dimethyl-formamide for 36h;

: 59277-89-3
acycloguanosine

: C20H33N3O9S

: (S)-2-((S)-2-tert-butoxycarbonylaminothiopropionylamino)succinic acid 4-[2-(2-amino-6-oxo-1,6-dihydropurin-9-ylmethoxy)ethyl] ester 1-tert-butyl ester

Conditions

Conditions	Yield
Stage #1: C20H33N3O9S With dicyclohexyl-carbodiimide In N,N-dimethyl-formamide at 0℃; for 1h; Inert atmosphere; Stage #2: acycloguanosine With dmap In N,N-dimethyl-formamide at 0 - 20℃; for 24h; Inert atmosphere;	96%

: 59277-89-3
acycloguanosine

: 81475-44-7
2-amino-8-bromo-9-[(2-hydroxyethoxy)methyl]-1,9-dihydro-6H-purin-6-one

Conditions

Conditions	Yield
With bromine In water at 20℃;	95%
With bromine In water at 20℃; for 0.5h;	87%
With bromine In water

: 59277-89-3
acycloguanosine

: 108-24-7
acetic anhydride

: 102728-64-3
9-[(acetoxyethoxy)methyl]guanine

Conditions

Conditions	Yield
With dmap In dimethyl sulfoxide for 0.166667h; Inert atmosphere;	95%
With dmap In DMF (N,N-dimethyl-formamide) at 20℃; for 18h;	91%
With pyridine at 40℃; for 2h;	78%
With pyridine; dmap In N,N-dimethyl-formamide for 36h;
With dmap

: 59277-89-3
acycloguanosine

: 13416-90-5
divinyl butanedioate

: succinic acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-ylmethoxy)-ethyl ester vinyl ester

Conditions

Conditions	Yield
With Candida antarctica lipase acrylic resin In acetone at 50℃; for 12h;	95%

: 59277-89-3
acycloguanosine

: 68-12-2, 33513-42-7
N,N-dimethyl-formamide

: 100699-59-0
N'-(9-((2-hydroxyethoxy)-methyl)-6-oxo-6,9-dihydro-1H-purin-2-yl)-N,N-dimethylformimidamide

Conditions

Conditions	Yield
In methanol at 20℃; for 96h;	95%

: 85-44-9
phthalic anhydride

: 59277-89-3
acycloguanosine

: C16H15N5O6

Conditions

Conditions	Yield
With triethylamine In N,N-dimethyl-formamide at 60℃; for 12h;	94.5%

: 59277-89-3
acycloguanosine

: 88950-64-5
1-<(tert-butyloxy)carbonylamino>cyclopropane-1-carboxylic acid

: 915725-88-1
1-tert-butoxycarbonylamino-cyclopropanecarboxylic acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-ylmethoxy)-ethyl ester

Conditions

Conditions	Yield
With dmap; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; triethylamine In N,N-dimethyl-formamide at 20℃;	94%
With dmap; N-(3-dimethylaminopropyl)-N-ethylcarbodiimide; triethylamine In N,N-dimethyl-formamide at 20℃;	93.7%

: 59277-89-3
acycloguanosine

: acyclovir hydrochloride

Conditions

Conditions	Yield
With hydrogenchloride In isopropyl alcohol at 20℃; for 0.5h;	94%

: 59277-89-3
acycloguanosine

: 55592-85-3
DL-N,N-di-CBZ-lysine

: 2,6-bis-benzyloxycarbonylamino-hexanoic acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-ylmethoxy)-ethyl ester

Conditions

Conditions	Yield
With dmap; dicyclohexyl-carbodiimide In N,N-dimethyl-formamide at 20℃; for 24h;	91%

: 59277-89-3
acycloguanosine

: 73-40-5
2-amino-1,9-dihydro-6H-purin-6-one

Conditions

Conditions	Yield
With sodium hydroxide In water	90%

: 59277-89-3
acycloguanosine

: 31233-28-0
diiodo(2,9-dimethyl-1,10-phenanthroline-κ(2)N,N')platinum(II)

: 75-09-2
dichloromethane

: [(9-(2-hydroxyethoxymethyl)-guanine)(2,9-dimethyl-1,10-phenantroline)PtI)I*5CH2Cl2

Conditions

Conditions	Yield
In methanol; dichloromethane soln. PtI2(Me2phen) (CH2Cl2) treated with soln of acyclovir (CH3OH); stirring for one day; solvent evapd. vac.; diethyl ether added; ppt. filtered; washed (ether);dried vac.; elem. anal.;	90%

...Expand

: 59277-89-3
acycloguanosine

: 31233-28-0
diiodo(2,9-dimethyl-1,10-phenanthroline-κ(2)N,N')platinum(II)

: 75-09-2
dichloromethane

: [(9-(2-hydroxyethoxymethyl)-guanine)2(2,9-dimethyl-1,10-phenantroline)Pt(II)]I2*CH2Cl2

Conditions

Conditions	Yield
In methanol; dichloromethane soln. PtI2(Me2phen) (CH2Cl2/CH3OH 1:1) treated with acyclovir; stirring for 2 h; solvent evapd. vac.; suspended (H2O); stirred over night; soln. filtered; evapd. vac.; elem. anal.;	90%

...Expand

Acyclovir Specification

1. Introduction of Acyclovir
Acyclovir is one kind of white to light yellow crystal powder. IUPAC Name of IUPAC Name is 2-Amino-9-(2-hydroxyethoxymethyl)-3H-purin-6-one. Product Category of Acyclovir is Active Pharmaceutical Ingredients;Purine;Nucleotides and Nucleosides;Antivirals for Research and Experimental Use;Biochemistry;Chemical Reagents for Pharmacology Research;Nucleosides, Nucleotides & Related Reagents. It can be soluble in water which is 0.7 mg/mL.

2. Properties of Acyclovir
Physical properties about Acyclovir are:
(1)Melting point: 256-257 °C; (2)Storage tempreture: -20 °C; (3)Water solubility: 0.7 mg/mL; (4)Index of Refraction: 1.762 ; (5)Density: 1.77 g/cm3 ; (6)Flash Point: 313.6 °C ; (7)Enthalpy of Vaporization: 93.25 kJ/mol ; (8)Boiling Point: 595 °C at 760 mmHg ; (9)Vapour Pressure: 5.29E-15 mmHg at 25 °C.

3. Structure Descriptors of Acyclovir
(1)InChI: InChI=1S/C8H11N5O3/c9-8-11-6-5(7(15)12-8)10-3-13(6)4-16-2-1-14/h3,14H,1-2,4H2,(H3,9,11,12,15);
(2)InChIKey: InChIKey=MKUXAQIIEYXACX-UHFFFAOYSA-N;
(3)Smiles: c1nc2c(=O)[nH]c(nc2n1COCCO)N.

4. Toxicity of Acyclovir
Aciclovir may cause nephrotoxicity (crystallization of aciclovir within renal tubules, elevation of serum creatinine, transient), and neurotoxicity (coma, hallucinations, lethargy, seizures, tremors). Nephrotoxicity and neurotoxicity usually resolve after cessation of aciclovir therapy. However, there is no well-defined relationship between aciclovir concentrations in the blood and these adverse effects.

Organism	Test Type	Route	Reported Dose (Normalized Dose)	Effect	Source
child	TDLo	oral	3gm/kg/22W-I (3000mg/kg)	BLOOD: AGRANULOCYTOSIS BLOOD: THROMBOCYTOPENIA	American Journal of Emergency Medicine. Vol. 16, Pg. 396, 1998.
mammal (species unspecified)	LD50	intravenous	400mg/kg (400mg/kg)		Pharmacy International. Vol. 5, Pg. 191, 1984.
man	TDLo	intravenous	134ug/kg/1D-I (0.134mg/kg)	BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS"	Lancet. Vol. 2, Pg. 385, 1985.
man	TDLo	intravenous	107mg/kg/4D-I (107mg/kg)	BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS" KIDNEY, URETER, AND BLADDER: "CHANGES IN TUBULES (INCLUDING ACUTE RENAL FAILURE, ACUTE TUBULAR NECROSIS)"	American Journal of Kidney Diseases. Vol. 22, Pg. 611, 1993.
man	TDLo	oral	486mg/kg/17D- (486mg/kg)	GASTROINTESTINAL: DECREASED MOTILITY OR CONSTIPATION GASTROINTESTINAL: OTHER CHANGES	American Journal of Gastroenterology. Vol. 88, Pg. 2110, 1993.
mouse	LD50	intraperitoneal	724mg/kg (724mg/kg)		Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 25, Pg. 815, 1994.
mouse	LD50	intravenous	1118mg/kg (1118mg/kg)		Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 16, Pg. 866, 1985.
mouse	LD50	oral	> 10gm/kg (10000mg/kg)		Nature. Vol. 272, Pg. 583, 1978.
mouse	LD50	subcutaneous	1118mg/kg (1118mg/kg)		Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 16, Pg. 866, 1985.
rat	LD50	intraperitoneal	860mg/kg (860mg/kg)		Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 16, Pg. 866, 1985.
rat	LD50	intravenous	750mg/kg (750mg/kg)		Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 25, Pg. 815, 1994.
rat	LD50	oral	> 20gm/kg (20000mg/kg)		Drugs in Japan Vol. -, Pg. 7, 1990.
rat	LD50	subcutaneous	620mg/kg (620mg/kg)		Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 16, Pg. 866, 1985.
women	LDLo	multiple routes	36mg/kg/2D-I (36mg/kg)	BRAIN AND COVERINGS: OTHER DEGENERATIVE CHANGES BEHAVIORAL: COMA LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES	American Journal of Kidney Diseases. Vol. 20, Pg. 647, 1992.
women	TDLo	intravenous	101mg/kg/2D-I (101mg/kg)	BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS" BEHAVIORAL: MUSCLE CONTRACTION OR SPASTICITY)	American Journal of Medicine. Vol. 94, Pg. 212, 1993.
women	TDLo	oral	12mg/kg/1D-I (12mg/kg)	BRAIN AND COVERINGS: MENINGEAL CHANGES BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) BEHAVIORAL: ANTIPSYCHOTIC	Southern Medical Journal. Vol. 87, Pg. 1227, 1994.
women	TDLo	oral	28mg/kg/2D-I (28mg/kg)	BRAIN AND COVERINGS: CHANGES IN SURFACE EEG BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS" LUNGS, THORAX, OR RESPIRATION: SPUTUM	Southern Medical Journal. Vol. 87, Pg. 1227, 1994.
women	TDLo	oral	80mg/kg/4D-I (80mg/kg)	BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS"	Annals of Internal Medicine. Vol. 111, Pg. 187, 1989.
women	TDLo	oral	100mg/kg/5D-I (100mg/kg)	SKIN AND APPENDAGES (SKIN): "DERMATITIS, ALLERGIC: AFTER SYSTEMIC EXPOSURE"	British Medical Journal. Vol. 289, Pg. 1424, 1984.

5. Physical Properties of Acyclovir

Physical Property	Value	Units	Temp (deg C)	Source
Melting Point	255	deg C		EXP
log P (octanol-water)	-1.56E+00	(none)		EXP
Water Solubility	1620	mg/L	22	EXP
Vapor Pressure	7.47E-15	mm Hg	25	EST
Henry's Law Constant	3.18E-22	atm-m3/mole	25	EST
Atmospheric OH Rate Constant	7.94E-11	cm3/molecule-sec	25	EST

6. Safety information of Acyclovir

Hazard Codes: Irritant Xi
Risk Statements: 36/37/38
R36/37/38: Irritating to eyes, respiratory system and skin.
Safety Statements: 22-24/25-36-26
S22: Do not breathe dust.
S24/25: Avoid contact with skin and eyes.
S26: In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
S36: Wear suitable protective clothing.

7. Uses of Acyclovir
Acyclovir is a commonly-used antiviral drug and is used for the treatment of herpes simplex virus infections. It is commonly marketed as tablets (200 mg, 400 mg, 800 mg and 1 gram), topical cream (5%), intravenous injection (25 mg/mL) and ophthalmic ointment (3%). It can be used especially against herpes.

Aciclovir (INN) or acyclovir is a synthetic deoxyguanosine analog and it is the prototype antiviral agent that is activated by viral thymidine kinase. The selective activity of aciclovir is due to its affinity for the thymidine kinase enzyme encoded by HSV and VZV.

8. Production of Acyclovir
(1)After Guanine trimethylsilyl and then react with 2-benzyloxyethoxy methyl chloride. Then remove the benzyl group to give acyclovir. The yield is 24%. The detailed steps are as follows:

(2)N, N'-diacetyl guanine and 2-oxa-butanediol diacetate in dimethyl sulfoxide can be used to manufacture the Acyclovir.

Production of Acyclovir

Product Name

Acyclovir

Synthetic route

Acyclovir Specification

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