Epinastine hydrochloride interMediate product

Base Information

• Chemical Name: Epinastine hydrochloride interMediate product
• CAS No.: 80012-79-9
• Molecular Formula: C₄H₄O₄*C₁₅H₁₆N₂
• Molecular Weight: 340.379
• Mol file: 80012-79-9.mol

Synonyms:Epinastine hydrochloride interMediate product

Chemical Property of Epinastine hydrochloride interMediate product

Chemical Property:

• Vapor Pressure: 4.48E-16mmHg at 25°C
• Boiling Point: 616.9°C at 760 mmHg
• Flash Point: 326.9°C
• PSA: 112.65000
• LogP: 3.25280

Purity/Quality:

98%,99%, ^*data from raw suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

Useful:

Technology Process of Epinastine hydrochloride interMediate product

There total 6 articles about Epinastine hydrochloride interMediate product which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 76.1%

N-<(11H-dibenzazepin-6-yl)methyl>phthalimide (74860-00-7) + (2E)-but-2-enedioic acid (110-17-8,26099-09-2) → 6,11-dihydro-5H-dibenzazepine-6-methanamine fumarate (127785-96-0,80012-79-9)

Guidance literature:

N-<(11H-dibenzazepin-6-yl)methyl>phthalimide; With sodium tetrahydroborate; In methanol; water; isopropyl alcohol; toluene; at 20 - 30 ℃; for 24.5h;

With hydrogenchloride; In water; isopropyl alcohol; at 20 - 80 ℃; for 1.5h;

(2E)-but-2-enedioic acid; With sodium hydroxide; more than 3 stages; Product distribution / selectivity;

Reference yield: 76.0%

6-aminomethyl-6,11-dihydro-5H-dibenzo[b,e]azepine (41218-84-2) + (2E)-but-2-enedioic acid (110-17-8,26099-09-2) → 6,11-dihydro-5H-dibenzazepine-6-methanamine fumarate (127785-96-0,80012-79-9)

Guidance literature:

In methanol; at 20 ℃; for 1h;

Reference yield:

N-[2-(phenylmethyl)phenyl]-2-chloroacetamide (21535-43-3) → 6,11-dihydro-5H-dibenzazepine-6-methanamine fumarate (127785-96-0,80012-79-9)

Guidance literature:

Multi-step reaction with 5 steps

1.1: trichlorophosphate / toluene / 6 h / 65 - 90 °C

2.1: potassium hydroxide / N,N-dimethyl-formamide / 55 °C

2.2: 15 h / 45 °C

3.1: formic acid; hydrogen; 5%-palladium/activated carbon / N,N-dimethyl-formamide / 24 h / 70 °C / 7500.75 Torr

4.1: hydrogenchloride / glycerol; water / 2.5 h / 20 - 110 °C

5.1: methanol / 1 h / 20 °C

With hydrogenchloride; formic acid; 5%-palladium/activated carbon; hydrogen; potassium hydroxide; trichlorophosphate; In methanol; water; N,N-dimethyl-formamide; glycerol; toluene;

upstream raw materials:

6-aminomethyl-6,11-dihydro-5H-dibenzo[b,e]azepine

(2E)-but-2-enedioic acid

N-<(11H-dibenzazepin-6-yl)methyl>phthalimide

N-[2-(phenylmethyl)phenyl]-2-chloroacetamide

Refernces

• 1、 -. "NOVEL CRYSTAL MODIFICATION OF EPINASTINE OR SALTS THEREOF AND PROCESS FOR PREPARATION THEREOF". Page/Page column 24. . Retrieved 2009/06/27.