41218-84-2

Basic information

• Product Name: 6-Aminomethyl-5,6-dihydromorphanthridine
• Synonyms: 6-Aminomethyl-6,11-dihydro-5H-dibenz [b,e]azepine hydrogen fumarate;Epinastine Related CoMpound A;6-(AMINOMETHYL)-6,11-DIHYDRO-DIBENZOAZEPINE;6,11-Dihydro-5H-dibenz[b,e]azepine-6-methanamine;6-Aminomethyl-5,6-dihydromorphanthridine
• CAS NO: 41218-84-2
• Molecular Formula: C₁₅H₁₆N₂
• Molecular Weight: 224.31
• Mol File: 41218-84-2.mol
• Article Data: 10

Chemical Properties

• Boiling Point: 401.9±24.0 °C(Predicted)
• Appearance: /
• Density: 1.096
• PKA: 9.42±0.29(Predicted)
• CAS DataBase Reference: 6-Aminomethyl-5,6-dihydromorphanthridine(CAS DataBase Reference)
• NIST Chemistry Reference: 6-Aminomethyl-5,6-dihydromorphanthridine(41218-84-2)
• EPA Substance Registry System: 6-Aminomethyl-5,6-dihydromorphanthridine(41218-84-2)

Safety Data

• Hazardous Substances Data: 41218-84-2(Hazardous Substances Data)

Usage

Uses

(6,?11-?Dihydro-?5H-?dibenzo[b,?e]?azepin-?6-?yl)?methanamine is an impurity of Epinastine (E588560), a tetracyclic, non-sedating histamine H1 receptor antagonist. Antihistaminic.

Upstream product

• 80012-69-7 11H-dibenzazepine-6-carbonitrile 
• 881036-44-8 6-cyano-azepine 
• 2835-77-0 (2-aminophenyl)(phenyl)methanone 
• 28059-64-5 2-benzylaniline 
• 15028-40-7 DL-2-phenylglycine methyl ester hydrochloride 
• 24461-61-8 phenylglycine methyl ester 
• 700-63-0 Phenylglycinamid 
• 1211-06-9 5,11-dihydro-6H-dibenz[b,e]azepin-6-one 
• 256-86-0 Morphanthridine 
• 147611-22-1 2-(benzylamino)benzaldehyde 
• 1143-50-6 5,6-dihydro-6,11-dioxomorphanthridine 
• 3311-41-9 5-benzyl-5,11-dihydro-6H-dibenzo[b,e]azepin-6-one 
• 449-55-8 6,11-dihydro-5H-dibenzo[b,e]azepine 

Downstream Products

• 127786-29-2 3-amino-9,13b-dihydro-1H-dibenzimidazo<1,5-a>azepine hydrobromide 
• 127785-96-0 6,11-dihydro-5H-dibenzazepine-6-methanamine fumarate 
• 80012-43-7 epinastine 
• 108929-04-0 epinastine hydrochloride 
• 71936-92-0 1,2,3,4,10,14b-hexahydrodibenzo[c,f]-pyrazino[1,2-a]azepine 
• 24219-97-4 mianserin 
• 127786-01-0 N-<(6,11-dihydro-5H-dibenzazepin-6-yl)methyl>-N'-ethyl-urea 
• 127786-00-9 N-<(6,11-dihydro-5H-dibenzazepin-6-yl)methyl>-N'-methyl-urea 
• 80012-85-7 1,2,9,13b-tetrahydro-3H-dibenzimidazo<1,5-a>azepine-3-thione 
• 127786-09-8 9,13b-dihydro-3-(4-morpholinyl)-1H-dibenzimidazo<1,5-a>azepine 
• 80012-87-9 9,13b-dihydro-N-pentyl-1H-dibenzimidazo<1,5-a>azepin-3-amine 
• 127786-10-1 9,13b-dihydro-3-(1-pyrrolidinyl)-1H-dibenzimidazo<1,5-a>azepine 

Relevant articles and documents

Synthetic method of epinastine hydrochloride

The invention relates to a synthesis method of epinastine hydrochloride. The method comprises the following steps: reacting phthalic anhydride with aniline to obtain a compound 1, reacting the compound 1 with polyphosphoric acid under certain conditions to perform cyclization to obtain a compound 2, reducing carbonyl of the compound 2 under certain conditions to obtain a compound 3, and carrying out chlorination reaction on the compound 3 to obtain a compound 4, carrying out cyano substitution reaction on the compound 4 to obtain a compound 5, reducing the compound 5 by using a carbon-nitrogenunsaturated bond to obtain a compound 6, reacting the compound 6 with cyanogen bromide, and forming hydrochloride by using hydrochloric acid to obtain a compound 7; according to the method, the epinastine hydrochloride is prepared from bulk chemical products, is extremely low in price and mild in reaction condition, avoids the use of azide compounds, and the method is suitable for large-scale industrial production. The prepared epinastine hydrochloride is high in purity and low in cost, and has higher market competitiveness.

A synthesis method of epinastine hydrochloride

The invention discloses a synthesis method for epinastine hydrochloride. With a compound (6-aminomethyl-6,11-dihydro-5H-dibenzo [b, e] azepine maleate), shown in the formula II, being the initial raw material, epinastine hydrochloride is synthesized. By the utilization of the synthesis method for epinastine hydrochloride, epinsastine hydrochloride can be effectively synthesized, and the method has the advantages of being high in synthesis efficiency, safe in production, simple in technology operation, short in production period and the like and is more suitable for large-scale and industrialized production of epinastine hydrochloride.

A 6 - aminomethyl - 6, 11 - dihydro - 5H - dibenzo [b, e] for the preparation method

The invention relates to a preparation method of 6-aminomethyl-6,11-dihydro-5H-dibenzo[b,e]azepine, and belongs to the technical field of drug synthesis. The preparation method comprises the following steps: (1) converting phenylglycine methyl ester hydrochloride into benzene ammonia amide through amidation reactions; (2) converting benzene ammonia amide into 2-((2-amino-2-oxo-phenethyl)amino)methyl benzoate through coupling reactions; (3) converting 2-((2-amino-2-oxo-phenethyl)amino)methyl benzoate into 2-((2-(hydroxymethyl)phenyl)amino)-2-phenyl acetamide through reduction reactions; (4) converting 2-((2-(hydroxymethyl)phenyl)amino)-2-phenyl acetamide into 6-aminomethyl-6,11-dihydro-5H-dibenzo[b,e]azepine through alkylation reactions. The provided preparation method has the advantage that no cyanide is used.