Dehydro-Silodosin Impurity

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E-mail: anna@molcoo.com.

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• Product Information

• Product Number: S013005

• English Name: Dehydro-Silodosin Impurity

• English Alias: (R)-1-(3-hydroxypropyl)-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)-1H-indole-7-carboxamide

• CAS Number: 175870-21-0

• Molecular Formula: C??H??F?N?O?

• Molecular Weight: 493.52

• Advantages

• As a dehydro impurity of Silodosin, this compound has the following advantages:
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• Well-defined and distinct structure: Contains indole carboxamide core, trifluoroethoxyphenoxyethylamino side chain, and hydroxypropyl group, differing from silodosin by the absence of specific double bond saturation. It can be accurately identified via HPLC and LC-MS, providing a specific marker for impurity detection;

• High stability and traceability: The synergistic effect of amide and ether bonds ensures high stability, and as a by-product of incomplete hydrogenation in silodosin synthesis, it directly reflects the efficiency of reduction steps, improving the accuracy of process tracing;

• High detection sensitivity: The strong electronegativity of trifluoromethyl and conjugated system of indole ring show characteristic UV absorption (270-290nm), combined with characteristic mass response (m/z 494 [M+H]?), enabling trace analysis via LC-MS, compatible with fluoroindole α? receptor antagonist detection systems.

• Applications

• Pharmaceutical quality control: Used as an impurity reference standard to identify and quantify Dehydro-Silodosin Impurity in silodosin APIs and formulations, ensuring residual dehydro impurities meet quality standards after hydrogenation;

• Synthesis process optimization: Optimizing hydrogenation conditions (e.g., catalyst activity, hydrogen pressure) by monitoring impurity content to improve selectivity of target saturated products and reduce dehydro by-products;

• Impurity profile enrichment: Contributing to the completeness of silodosin’s impurity profile, providing key data for comprehensive evaluation of drug purity and potential safety risks, supporting drug quality research and regulatory submissions.

• Background Description

• Silodosin is a selective α?A adrenergic receptor antagonist used to treat benign prostatic hyperplasia, with a structure including an indole ring, trifluoroethoxyphenoxy side chain, and saturated aminopropyl group. During synthesis, incomplete hydrogenation of unsaturated bonds in the indole ring side chain may generate derivatives retaining partial unsaturated structures, namely Dehydro-Silodosin Impurity. The presence of this impurity may affect the stability and biological activity of the drug, so its control is an important part of silodosin quality assurance.

• Research Status

• Current research focuses on:
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• Detection method advancement: Developing UPLC-MS/MS methods to achieve simultaneous quantification of the impurity and silodosin in complex matrices by utilizing fragment ion differences (such as characteristic cleavage of unsaturated bonds), with a detection limit as low as 0.1 ppb;

• Hydrogenation mechanism analysis: Studying the formation kinetics of the impurity by simulating different catalyst types and reaction temperatures to clarify the key influencing factors of silodosin side chain hydrogenation;

• Activity evaluation: Comparing the receptor affinity between this impurity and silodosin through in vitro α?A receptor binding experiments to evaluate its potential impact on drug efficacy;

• Process stability verification: Establishing a monitoring system for this impurity in large-scale production to ensure the stability and reproducibility of the hydrogenation process and reduce batch-to-batch fluctuations in impurity content

This product is intended for laboratory use only!

WhatsAPP: +86 17386083646
E-mail: anna@molcoo.com