Olopatadine

Base Information

• Chemical Name: Olopatadine
• CAS No.: 113806-05-6
• Molecular Formula: C21H23NO3
• Molecular Weight: 337.419
• Mol file: 113806-05-6.mol

Synonyms:Dibenz[b,e]oxepin-2-aceticacid, 11-[3-(dimethylamino)propylidene]-6,11-dihydro-, (Z)-;11-[(Z)-3-(Dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-aceticacid;Opatanol;Pataday;Patanol;

Chemical Property of Olopatadine

Chemical Property:

• Appearance/Colour: white or off-white crystalline powder
• Melting Point: 188-189.5°
• Boiling Point: 523 °C at 760 mmHg
• Flash Point: 270.1 °C
• PSA: 49.77000
• Density: 1.221 g/cm³
• LogP: 3.58950
• Storage Temp.: Amber Vial, Refrigerator
• Solubility.: Chloroform (Slightly, Heated), DMSO (Slightly)

Purity/Quality:

99% ^*data from raw suppliers

Olopatadine ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Total 1 MSDS from other Authors

Useful:

• Description: Olopatadine belongs to a kind of antihistamine reagent. It is a relatively selective H1-receptor antagonist and can inhibit the histamine release process from the mast cell, subsequently leading to temporary relief on the negative symptoms associated with histamine. It is devoid of effects on alpha-adrenergic, dopamine and muscarinic type I and II receptors. Its 0.1% solution can be used for topical administration to the eyes. It is indicated for the treatment of itching associated with allergic conjunctivitis.
• Uses: Olopatadine is a dual acting histamine H1-receptor antagonist and mast cell stabilizer. Antiallergic; antihistaminic. Anti-allergic.
• Therapeutic Function: Antiallergic

Technology Process of Olopatadine

There total 24 articles about Olopatadine 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: 96.09%

(Z)-11-(3-dimethylaminopropylidene)-6,11-dihydro-dibenz-[b,e]oxepine-2-acetic acid hydrobromide (951006-73-8) → olopatadine (113806-05-6)

Guidance literature:

With sodium hydroxide; In water; at 5 - 25 ℃; for 20 - 21.0833h; pH=6.8 - 7.2; Product distribution / selectivity;

Reference yield: 92.0%

(Z)-11-<3-(dimethylamino)propylidene>-6,11-dihydrodibenzoxepin-2-acetic acid methyl ester (113806-01-2) → olopatadine (113806-05-6)

Guidance literature:

(Z)-11-<3-(dimethylamino)propylidene>-6,11-dihydrodibenzoxepin-2-acetic acid methyl ester; With methanol; sodium hydroxide; water; at 20 ℃; for 5h;

With hydrogenchloride; In methanol; water;

In methanol; water;

Reference yield: 81.2%

isoxepac (55453-87-7) + N,N-dimethyl-3-bromopropylamine (53929-74-1) → olopatadine (113806-05-6)

Guidance literature:

N,N-dimethyl-3-bromopropylamine; With zinc dibromide; In tetrahydrofuran; at 10 - 20 ℃; for 0.166667h; Inert atmosphere;

With naphthalene; lithium; In tetrahydrofuran; at 65 - 70 ℃; Inert atmosphere;

isoxepac; In tetrahydrofuran; at 0 - 25 ℃; for 16.5h; Reagent/catalyst; Temperature;

upstream raw materials:

(Z)-11-<3-(dimethylamino)propylidene>-6,11-dihydrodibenzoxepin-2-acetic acid methyl ester

(Z)-11-(3-dimethylaminopropylidene)-6,11-dihydro-dibenz-[b,e]oxepine-2-acetic acid hydrobromide

11-[(Z)-3-(dimethylamino)-propylidene]-6,11-dihydrodibenzo[b,e]oxepin-2-acetamide p-toluensulfonate

(Z)-11-[3-(dimethylamino)propylidene]-6,11-dihydro-dibenz[b,e]oxepin-2-acetic acid butyl ester

Downstream raw materials:

(Z)-11-<3-(dimethylamino)propylidene>-2-(2-hydroxyethyl)-6,11-dihydrodibenzoxepin

olopatadine hydrochloride

Refernces

• 1、 Endoori,Gulipalli, K. Ch.,Bodige,Seelam. "Novel and Efficient Synthesis of Deuterium-Labeled Olopatadine-d6". . p. 1387 - 1393. Retrieved 2019/11/03.
• 2、 -. "A process for the preparation of olopatadine hydrochloride". Paragraph 0057; 0058. . Retrieved 2016/10/08.