Delving into the Latest Updates on SB-214111 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

5-HT6 receptor

Mechanism

5-HT6 receptor antagonists(Serotonin 6 (5-HT6) receptor antagonists)

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Central Nervous System Diseases

Originator Organization

Smithkline Beecham Plc

Active Organization-

Inactive Organization

Smithkline Beecham Plc

Drug Highest PhaseDiscontinuedDiscovery

First Approval Date-

Regulation-

Structure

Molecular FormulaC18H22BrN3O3S

InChIKeyOZYPUQNRUYTZDI-UHFFFAOYSA-N

CAS Registry209480-37-5

AbstractReversing the conventional site‐selectivity of C−H activation provides efficient retrosynthetic disconnections to otherwise unreactive bonds. Described herein is the Brønsted acid‐catalyzed reaction that selectively performs meta‐amination of anisidines with aliphatic‐, heterocyclic‐ and aromatic amines in a one‐pot procedure. In addition to dramatically simplifying the synthesis of meta‐substituted anilines, our approach has the advantage of the scalability and remarkable functional group tolerance, including late‐stage functionalization of pharmaceutical compounds and natural products. The control experiments and detailed computational analysis provide insight into the reaction mechanism and the origin of meta‐selectivity. The protocol extended to the synthesis of challenging tri‐aminated arenes and successfully applied for the efficient synthesis of 5‐HT6 receptor antagonists, the anti‐psychotic drugs viz.. SB‐214111, SB‐258510, and specifically, anti‐schizophrenic drug SB‐271046.

100 Deals associated with SB-214111

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