Conditions | Yield |
---|---|
With 10-methyl-9-(2,4,6-trimethylphenyl) acridinium tetrafluoroborate In acetonitrile at 20℃; for 5h; Irradiation; | 76% |
5-acetamido-1,3,4-thiadiazolyl-2-sulfonyl chloride
acetazolamide
Conditions | Yield |
---|---|
With 1,1,1-triphenylsilylamine In acetonitrile for 1h; Reflux; Inert atmosphere; | 74% |
With ammonium hydroxide In water for 1h; Cooling with ice; | 72% |
With ammonium hydroxide at 20℃; for 0.5h; | 46% |
2-acetylamino-5-benzylmercapto-1,3,4-thiadiazole
acetazolamide
Conditions | Yield |
---|---|
With chlorine; acetic acid anschliessendes Behandeln mit fluessigem NH3; | |
Stage #1: 2-acetylamino-5-benzylmercapto-1,3,4-thiadiazole With chlorine; acetic acid at 50℃; for 0.5h; Stage #2: With ammonia | |
Stage #1: 2-acetylamino-5-benzylmercapto-1,3,4-thiadiazole With water; chlorine; acetic acid at 5℃; for 0.5h; Stage #2: With ammonia |
Conditions | Yield |
---|---|
With water at 37℃; pH=7.4; |
Conditions | Yield |
---|---|
With water at 37℃; pH=7.4; |
Conditions | Yield |
---|---|
With water at 37℃; pH=7.4; |
acetazolamide
5-amino-1, 3, 4-thiadiazole-2-sulfonamide
Conditions | Yield |
---|---|
With hydrogenchloride In ethanol for 4h; Reflux; | 100% |
With hydrogenchloride In methanol; water for 18h; Reflux; | 98% |
With hydrogenchloride; water In methanol for 18h; Reflux; | 98% |
acetazolamide
Conditions | Yield |
---|---|
With sodium hydroxide In water at 55℃; for 2h; | 99% |
Conditions | Yield |
---|---|
With NH3 In ethanol addn. of the ligand to a soln. of CoCl2 in ethanol, warming, stirring, addn. of NH3; filtn. of ppt., washing (EtOH), dried at 40 °C, elem. anal.; | 98% |
acetazolamide
5-amino-2-sulfamoyl-1,3,4-thiadiazole monohydrochloride
Conditions | Yield |
---|---|
With hydrogenchloride for 3h; Reflux; | 96% |
With hydrogenchloride In water for 3h; Reflux; | 96% |
With hydrogenchloride for 3h; Reflux; | 96% |
With hydrogenchloride In ethanol for 3h; Inert atmosphere; Reflux; | 65% |
With hydrogenchloride; water at 60℃; for 2h; Heating / reflux; |
Conditions | Yield |
---|---|
With NH3 In methanol addn. of NH3 to a soln. of ligand in methanol, addn. of ZnCl2, stirring, pptn. on standing at room temp. for 3 h; filtn., washing (water), drying at 60°C, elem. anal.; | 96% |
Conditions | Yield |
---|---|
In ethanol solid ligand was dissolved in hot soln. of CuBr2 in EtOH with heating and stirring, propanediamine was added dropwise with stirring; soln. was stored at 4°C for 3-4 d, crystals were collected, elem. anal.; | 90% |
[ruthenium(II)(η6-1-methyl-4-isopropyl-benzene)(chloride)(μ-chloride)]2
acetazolamide
Conditions | Yield |
---|---|
In acetone for 7h; Reflux; | 90% |
In acetone at 20℃; for 12h; Temperature; | 47% |
acetazolamide
Conditions | Yield |
---|---|
In methanol; chloroform | 87% |
In methanol; chloroform | 87% |
Conditions | Yield |
---|---|
With NH3 In ammonia NH3 (liquid); dissolving of the ligand and the Zn-salt in NH3, dropwise combining of the both soln.; slow evapn. of NH3 for 2 months; | 87% |
[ruthenium(II)(η6-1-methyl-4-isopropyl-benzene)(chloride)(μ-chloride)]2
acetazolamide
Conditions | Yield |
---|---|
With sodium hydroxide In methanol; water at 20℃; for 16h; | 86% |
Conditions | Yield |
---|---|
With sodium hydroxide at 8℃; pH=8.5 - 9.5; | 82% |
Conditions | Yield |
---|---|
With sodium hydroxide at 8℃; pH=8.5 - 9.5; | 82% |
Conditions | Yield |
---|---|
With sodium hydroxide at 8℃; pH=8.5 - 9.5; | 81% |
Conditions | Yield |
---|---|
With sodium hydroxide at 8℃; pH=8.5 - 9.5; | 81% |
Conditions | Yield |
---|---|
In water for 0.0416667h; Time; Microwave irradiation; Green chemistry; | 79% |
Conditions | Yield |
---|---|
With sodium hydroxide at 8℃; pH=8.5 - 9.5; | 78% |
acetazolamide
Conditions | Yield |
---|---|
In methanol; dichloromethane; water stirred at room temp. for 1 d in a solvent mixture of CH2Cl2/CH3OH/H2O=10/8/3; solvent removed in vac.; recrystd. (methanol) at -25°C; elem. anal.; | 76% |
Conditions | Yield |
---|---|
With sodium hydroxide at 8℃; pH=8.5 - 9.5; | 75% |
Conditions | Yield |
---|---|
With sodium hydroxide at 8℃; pH=8.5 - 9.5; | 75% |
Conditions | Yield |
---|---|
With sodium hydroxide In 1,4-dioxane; water at 8℃; pH=7 - 9.5; | 70% |
Conditions | Yield |
---|---|
With sodium hydroxide at 8℃; pH=8.5 - 9.5; | 68% |
Conditions | Yield |
---|---|
With sodium hydroxide In 1,4-dioxane; water at 8℃; pH=7 - 9.5; | 65% |
acetazolamide
Conditions | Yield |
---|---|
With NaOH; diethylenetriamine In methanol addn. of stoich. amt. of acetazolamide soln. contg. 1 equiv. of NaOH to Cu(ClO4)2, stirring (several min), dropwise addn. of diethylenetriamine,(stirring, pptn.); filtration, washing (MeOH), drying; elem. anal.; | 62% |
Conditions | Yield |
---|---|
In ethanol heated, stirred, ethanediamine was added dropwise with stirring; filtered (violet product), soln. was stored at room temp. for 4-24 h, crystals (purple) were collected, elem. anal.; | A 60% B 30% |
Conditions | Yield |
---|---|
With sodium hydroxide In 1,4-dioxane; water at 8℃; pH=7 - 9.5; | 55% |
Conditions | Yield |
---|---|
In methanol; water for 4h; Reflux; | 54% |
In methanol; water for 4h; Reflux; |
Conditions | Yield |
---|---|
With caesium carbonate In N,N-dimethyl-formamide at 20℃; for 16h; | 45.3% |
Conditions | Yield |
---|---|
In acetonitrile dropwise addn. of soln. of Zn(ClO4)2*6H20 and acetazolamide to soln. of (12)aneN3 in MeCN; filtration, crystn. on evapn. (slow, room temp.); elem. anal.; | 40% |
The Acetazolamide has the cas register number 59-66-5, and its IUPAC name is N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide. It belongs to the product category which is Miscellaneous Enzyme.
This is a kind of white to yellowish-white fine crystalline powder with no odor or taste. Besides, it is slightly soluble in water, ethanol, nearly insoluble in chloroform and ethyl ether, and easily soluble in ammonia solution.
The characteristics of this chemical are as follows: (1)ACD/LogP: -0.26; (2)ACD/LogD (pH 5.5): -0.26; (3)ACD/LogD (pH 7.4): -0.48; (4)ACD/BCF (pH 5.5): 1; (5)ACD/BCF (pH 7.4): 1; (6)ACD/KOC (pH 5.5): 17.06; (7)ACD/KOC (pH 7.4): 10.47; (8)#H bond acceptors: 7; (9)#H bond donors: 3; (10)#Freely Rotating Bonds: 1; (11)Polar Surface Area: 120.09; (12)Index of Refraction: 1.64; (13)Molar Refractivity: 45.95 cm3; (14)Molar Volume: 127.3 cm3; (15)Polarizability: 18.21 ×10-24 cm3; (16)Surface Tension: 97.9 dyne/cm; (17)Density: 1.744 g/cm3.
The production method of Acetazolamide: It could be produce from the amination. Firstly, mix the ammonia water and trash ice till the temperature cools to below 5℃, and then add oxychloride to have heat preservation reation for about half an hour; Secondly, adjust PH to 5-6 with hydrochloric acid and then filter with filter cake to have the PH7, and then dry to get the acetazolamide crude products; Thirdly, heat the mixture of crude products, water, activated carbon and Na2S2O5 to 95℃, and then go through the decoloration for 1-1.5hour to get crystal after filtering and cooling; Lastly, have a listing process of filtering, washing and drying to get the products.
Use of Acetazolamide: Acetazolamide reacts to produce 5-amino-[1,3,4]thiadiazole-2-sulfonic acid amide, with the following condition: reagent: HCL (37 percent); reaction time: 2 hours; yield: 2.75g; other condition: heating.
As to its usage, it is widely applied in pharmeceutics. It is a kind of diuretic, and also as carbonic anhydrase inhibitor to resist carbonic anhydrase in kidney tubules epithelial cell; It has the function of controlling Aqueous Humour secretion to release the intraocular tension, which could be applied in curing glaucoma and mild cardiac edema.
In addition, you could obtain the molecular structure by converting the following datas:
(1)SMILES:O=S(=O)(c1nnc(s1)NC(=O)C)N
(2)InChI:InChI=1/C4H6N4O3S2/c1-2(9)6-3-7-8-4(12-3)13(5,10)11/h1H3,(H2,5,10,11)(H,6,7,9)
(3)InChIKey:BZKPWHYZMXOIDC-UHFFFAOYAA
Below are the toxicity information of this chemical:
Organism | Test Type | Route | Reported Dose (Normalized Dose) | Effect | Source |
---|---|---|---|---|---|
dog | LD50 | intravenous | > 2gm/kg (2000mg/kg) | Drugs in Japan Vol. 6, Pg. 15, 1982. | |
guinea pig | LD50 | subcutaneous | > 1500mg/kg (1500mg/kg) | Drugs in Japan Vol. 6, Pg. 15, 1982. | |
man | TDLo | oral | 54mg/kg/5D-I (54mg/kg) | LUNGS, THORAX, OR RESPIRATION: DYSPNEA | Archives of Internal Medicine. Vol. 143, Pg. 1278, 1983. |
mouse | LD50 | intraperitoneal | 1175mg/kg (1175mg/kg) | Russian Pharmacology and Toxicology Vol. 39, Pg. 255, 1976. | |
mouse | LD50 | intravenous | > 3gm/kg (3000mg/kg) | Drugs in Japan Vol. 6, Pg. 15, 1982. | |
mouse | LD50 | oral | 4300mg/kg (4300mg/kg) | Acta Biologica et Medica Germanica. Vol. 21, Pg. 193, 1968. | |
mouse | LD50 | subcutaneous | > 3gm/kg (3000mg/kg) | Drugs in Japan Vol. 6, Pg. 15, 1982. | |
rat | LD50 | intraperitoneal | 2750mg/kg (2750mg/kg) | Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. Vol. 56(4), Pg. 134S, 1960 |
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