Bepotastine Besilate

Base Information

• Chemical Name: Bepotastine Besilate
• CAS No.: 190730-42-8
• Molecular Formula: C21H25ClN2O3.C6H6O3S
• Molecular Weight: 0
• Mol file: 190730-42-8.mol

Synonyms:1-Piperidinebutanoic acid, 4-[(4-chlorophenyl)-2-pyridinylmethoxy]-, (R)-, monobenzenesulfonate;(R)-4-[(4-Chlorophenyl)-2-pyridinylmethoxy]-1-piperidinebutanoic acid monobenzenesulfonate

Chemical Property of Bepotastine Besilate

Chemical Property:

• Vapor Pressure: 8.63E-13mmHg at 25°C
• Boiling Point: 546.8°C at 760 mmHg
• Flash Point: 284.5°C
• PSA: 125.41000
• LogP: 6.12220

Purity/Quality:

98% ^*data from raw suppliers

(R)-BepotastineBesylate ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

Useful:

• Uses: (R)-Bepotastine Besylate is the R-isomer of (S)-Bepotastine Besylate (B317000); a histamine H1 receptor antagonist. Bepotastine suppresses some allergic inflammatory processes such as allergic rhinitis, chronic urticaria or pruritus associated with skin conditions (eczema/dermatitis, prurigo or pruritus cutaneus).

Technology Process of Bepotastine Besilate

There total 42 articles about Bepotastine Besilate 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: 99.9%

benzenesulfonic acid (98-11-3) + Bepotastine (125602-71-3,190786-43-7,190730-41-7) → [14C]-Bepotastine besilate (125602-71-3,190786-44-8,190730-42-8)

Guidance literature:

In ethanol; at 50 ℃;

DOI:10.1080/00304948.2020.1868930

Reference yield: 75.0%

(S)-(-)-2-((4-chlorophenyl)(piperidin-4-yloxy)methyl)pyridine (210095-55-9) + Ethyl 4-bromobutyrate (2969-81-5) + benzenesulfonic acid (98-11-3) → [14C]-Bepotastine besilate (125602-71-3,190786-44-8,190730-42-8)

Guidance literature:

(S)-(-)-2-((4-chlorophenyl)(piperidin-4-yloxy)methyl)pyridine; Ethyl 4-bromobutyrate; With potassium carbonate; In acetonitrile; at 60 ℃; for 6h; Large scale;

With sodium hydroxide; In acetonitrile; at 20 ℃; for 2h; Large scale;

benzenesulfonic acid; In acetonitrile; at 70 ℃; Solvent; Temperature; Large scale;

Reference yield: 67.3%

benzene-sulfonic acid monohydrate (26158-00-9,5928-72-3) + Bepotastine (125602-71-3,190786-43-7,190730-41-7) → [14C]-Bepotastine besilate (125602-71-3,190786-44-8,190730-42-8)

Guidance literature:

In ethyl acetate;

upstream raw materials:

benzenesulfonic acid

Bepotastine

bepotastine besilate

4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidine

Refernces

• 1、 -. "Total synthesis method of bestatin". Paragraph 0020; 0050; 0064-0066; 0066; 0080-0081. . Retrieved 2021/10/11.
• 2、 -. "A stable besylate bepotastine crystal and its preparation method". Paragraph 0054-0055. . Retrieved 2018/02/04.