Introduction：Basic information about AZATADINE MALEATE (200 MG) CAS 3978-86-7, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
AZATADINE MALEATE (200 MG) Basic information
| Product Name: | AZATADINE MALEATE (200 MG) |
| Synonyms: | AZATADINE MALEATE;OPTIMINE;ZADINE;Zadine;11h-benzo(5,6)cyclohepta(1,2-b)pyridine,5,6-dihydro-11-(1-methyl-4-piperidylid;6,11-dihydro-11-(1-methyl-4-piperidylidene)5h-benzo(5,6)cyclohepta(1,2-b)pyr;azatadinedimaleate;5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-, (2Z)-2-butenedioate (1:2);Azatadine Maleate(Azatadine dimaleate);azatadinemaleate |
| CAS: | 3978-86-7 |
| MF: | C28H30N2O8 |
| MW: | 522.5464 |
| EINECS: | 223-615-8 |
| Product Categories: | |
| Mol File: | 3978-86-7.mol |
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AZATADINE MALEATE (200 MG) Chemical Properties
| Melting point | 152-154° |
| storage temp. | Sealed in dry,Room Temperature |
| solubility | DMSO (Slightly), Methanol (Slightly) |
| form | Solid |
| color | White to Off-White |
Safety Information
AZATADINE MALEATE (200 MG) Usage And Synthesis
| Chemical Properties | White Solid |
| Originator | Idulian,Unilabo,France,1968 |
| Uses | Antihistaminic. |
| Definition | ChEBI: The dimaleate salt of azatadine. |
| Manufacturing Process | Preparation of 4-aza-5-(N-methyl-4-piperidyl)-10,11-dihydro-5Hdibenzo[a,d]cycloheptene-5-ol: Add 17.4 g of N-methyl-4-chloropiperidine to astirred mixture containing 3.2 g of magnesium, 20 ml of anhydroustetrahydrofuran, 1 ml of ethyl bromide and a crystal of iodine. Reflux for twohours, cool to 30-35°C and add a solution of 13 g of 4-aza-10,11-dihydro-5Hdibenzo[a,d]cycloheptene-5-one in 25 ml of tetrahydrofuran. Stir for fivehours, remove the solvent by distillation in vacuum and add 250 ml of ether.Add 100 ml of 10% ammonium chloride solution and extract the mixture withchloroform. Concentrate the chloroform solution to a residue and recrystallizefrom isopropyl ether obtaining 20 g of the carbinol, MP 173-174°C.
Preparation of 4-aza-5-(N-methyl-4-piperidylidene)-10,11-dihydro-5Hdibenzo[a,d]cycloheptene: Heat 5.4 g of the carbinol and 270 g ofpolyphosphoric acid for 12 hours at 140-170°C. Pour into ice water and makealkaline with sodium hydroxide. Extract with ether. Dry ether solution andconcentrate to a residue. Crystallize from isopropyl ether, MP 124-126°C.
Preparation of 4-aza-5-(N-methyl-4-piperidylidene)-10,11-dihydro-5Hdibenzo[a,d]cycloheptene dimaleate: To a solution containing 4.3 g of 4-aza-(N-methyl-4-piperidylidene)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene in 55ml of ethyl acetate, add a solution of 3.45 g of maleic acid dissolved in ethylacetate. Filter the resulting precipitate and recrystallize the desired productfrom an ethyl acetate-methanol mixture to yield 4-aza-5-(N-methyl-4-piperidylidene)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene dimaleate, MP152-154°C. |
| Brand name | Optimine (Schering);Verban. |
| Therapeutic Function | Antihistaminic |
| General Description | Azatadine maleate, 6,11-dihydro-11-(l-methyl-4-piperidylidene)-5H-benzo-[5,6]cyclo-hepta(1,2-b]pyridine maleate (1:2) (Optimine), is a potent,long-acting antihistaminic with antiserotonin activity. Inearly testing, azatadine exhibited more than three times thepotency of chiorpheniramine in the isolated guinea pigileum screen and more than seven times the oral potency ofchlorpheniramine in protection of guinea pigs against a doublelethal dose of intravenously administered histamine. |
AZATADINE MALEATE (200 MG) Preparation Products And Raw materials
| Raw materials | Magnesium-->Bromoethane-->Polyphosphoric acid-->Maleic acid-->4-Chloropiperidine hydrochloride |
