Delving into the Latest Updates on Troxipide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Troxipide (JP17/INN), 曲昔派特

+ [3]

Target-

Action-

Mechanism-

Therapeutic Areas

Digestive System Disorders

Active Indication

Acute gastritisChronic gastritisStomach Ulcer

Inactive Indication-

Originator Organization

KYORIN Pharmaceutical Co., Ltd.

Active Organization

KYORIN Pharmaceutical Co., Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (30 Apr 1986),

Stomach Ulcer

Regulation-

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Structure/Sequence

Molecular FormulaC15H22N2O4

InChIKeyYSIITVVESCNIPR-UHFFFAOYSA-N

CAS Registry30751-05-4

The incorporation of aromatic difluoromethyl motifs has proven to be a fruitful strategy for enhancing the therapeutic profiles of modern pharmaceutical candidates. While the defluorofunctionalization of trifluoromethylarenes offers a promising pathway toward diverse aromatic difluoromethyl compounds, current methods are predominantly limited to two-component reactions. Multicomponent cascade reactions (MCRs) involving a transient aromatic difluoromethyl radical are still uncommon and highly sought after, owing to their capacity to rapidly generate challenging molecular structures. In this study, we present a photocatalytic manifold that combines commercially available trifluoromethylarenes, feedstock dienes, and various nucleophiles to achieve a modular defluorinative MCR. This method features mild reaction conditions and a broad substrate scope with excellent functional group compatibility. Furthermore, this protocol enables a previously unreported process of defluorinative editing for the resulting MCR aromatic difluoromethyl adducts. Preliminary mechanistic studies support the proposed photoexcited palladium catalytic cycle.

23 Sep 2024·Angewandte Chemie International Edition

Visible‐Light‐Driven Multicomponent Reactions for the Versatile Synthesis of Thioamides by Radical Thiocarbamoylation

Article

Author: Wang, Jia‐Jin ; Wu, Xuesong ; Wang, Jia-Jin ; Xiong, Yanjiao ; Guo, Hong-Mei ; Guo, Hong‐Mei

AbstractThioamides are widely used structures in pharmaceuticals and agrochemicals, as well as important synthons for the construction of sulfur‐containing heterocycles. This report presents a series of visible‐light‐driven multicomponent reactions of amines, carbon disulfide, and olefins for the mild and versatile synthesis of linear thioamides and cyclic thiolactams. The use of inexpensive and readily available carbon disulfide as the thiocarbonyl source in a radical pathway enables the facile assembly of structurally diverse amine moieties with non‐nucleophilic carbon‐based reaction partners. Radical thiocarbamoylative cyclization provides a practical protocol that complements traditional approaches to thiolactams relying on deoxythionation. Mechanistic studies reveal that direct photoexcitation of in situ formed dithiocarbamate anions as well as versatile photoinduced electron transfer with diverse electron acceptors are key to the reactions.

04 Sep 2024·Journal of the American Chemical Society

Versatile, Modular, and General Strategy for the Synthesis of α-Amino Carbonyls

Article

Author: Liu, Jianzhong ; Gaunt, Matthew J.

Modulating the basicity of alkylamines is a crucial factor in drug design. Consequently, alkylamines with a proximal amide, ester, or ketone have become privileged features in many pharmaceutical candidates. The impact of α-amino carbonyls has made the development of new methods for their preparation a continuous challenge in synthesis. Here, we describe a practical strategy that provides a modular and programmable synthesis of a wide range of α-amino carbonyls. The generality of this process is made possible by an extremely mild method to generate carbamoyl radicals, proceeding via a Lewis acid-visible-light-mediated Norrish type-I fragmentation of a tailored carboxamide reagent and intercepted through addition to in situ generated unbiased imines. Aside from the reaction's broad scope in each component, its capacity to draw on plentiful and diversely populated amine and carbonyl feedstocks is showcased through a two-dimensional array synthesis that is used to construct a library of novel, assay-ready, α-amino amides.

100 Deals associated with Troxipide

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External Link

KEGG	Wiki	ATC	Drug Bank
D01306	Troxipide	A02BX11	DB13419

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Acute gastritis	Japan	KYORIN Pharmaceutical Co., Ltd.	04 Sep 1991
Chronic gastritis	Japan	KYORIN Pharmaceutical Co., Ltd.	04 Sep 1991
Stomach Ulcer	Japan	KYORIN Pharmaceutical Co., Ltd.	30 Apr 1986