Delving into the Latest Updates on KW-4099 with Synapse

Overview

Basic Info

Drug Type

Unknown

Synonyms

Target

TBXA2R

Mechanism

TBXA2R antagonists(Thromboxane A2 receptor antagonists)

Therapeutic Areas

Respiratory Diseases

Active Indication-

Inactive Indication

Respiratory Diseases

Originator Organization

Kyowa Kirin Co., Ltd.

Active Organization-

Inactive Organization

Kyowa Kirin Co., Ltd.

Drug Highest PhaseDiscontinuedPreclinical

First Approval Date-

Regulation-

Methyl (+/-)-11-(2-hydroxyethyl)thio-6,11-dihydrodibenz[b,e]oxepin- 2- carboxylate (5) was enantio-selectively acylated with acetic anhydride in an organic medium by Lipase Amano P to give methyl (-)-11-(2-acetoxyethyl)thio-6,11-dihydrodibenz[b,e]oxepin-2- carboxylate (8), and the (+)-enantiomer by Lipase Sigma Type VII. Using Lipase Amano P, (+)- and (-)-(5) could be prepared with high optical purity (84-94% e.e.). These products were respectively converted to (+)- and (-)-KW-4099, which had antiallergic activity with complete retention of the optical purity.

01 Jan 1992·Chemical and Pharmaceutical BulletinQ4 · MEDICINE

Synthesis and Optical Resolution of an Antiallergic Agent KW4099 with Thromboxane A2 Antagonistic Activity.

Q4 · MEDICINE

Article

Author: Tomioka, Shinji ; Sugaya, Toru ; Tamaki, Kentaro ; Kuge, Yukihiro

A new antiallergic agent with thromboxane A2 antagonistic activity, KW4099, was synthesized by a simple method. Its optical resolution was accomplished with the use of (+)- or (-)-2,2'-(1,1'-binaphthyl)phosphoric acid as a resolving agent.

100 Deals associated with KW-4099

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