Keywords

• Rimegepant Impurity (Dihydrochloride)
• 1373116-08-5
• C10H16N4·2HCl

Quick Details

• ProName: Rimegepant Impurity (Dihydrochloride);...
• CasNo: 1373116-08-5
• Molecular Formula: C10H16N4·2HCl
• Appearance: White to off white powder
• Application: experiment research
• DeliveryTime: prompt delivery
• PackAge: Food bags, aluminum foil bags
• Port: Shenzhen/hongkong
• ProductionCapacity: 5000 Gram/Year
• Purity: 99%+ HPLC
• Storage: cool and dry
• Transportation: DHL,EMS,TNT,UPS,EMS,by air,by sea;
• LimitNum: 10 Milligram
• Moisture Content: 0.1%
• Impurity: 0.1%

Superiority

Advantages

• High-Purity Reference Standard：Confirmed by HPLC (≥99.0%), NMR (1H, 13C), HRMS, and elemental analysis, suitable for Rimegepant impurity analysis and quality control.

• Stability Assurance：Stable for 36 months at -20℃ under light-protected, sealed storage; degradation rate <0.3% in aqueous solution within 6 months.

Details

Rimegepant Impurity (Dihydrochloride); 1373116-08-5

Product Information

• Product Code：R046084A

• English Name：Rimegepant Impurity 84(Dihydrochloride)

• English Alias：852627-75-9(free base); N³-(piperidin-4-yl)pyridine-2,3-diamine dihydrochloride

• CAS No.：1373116-08-5

• Molecular Formula：C??H??N?·2HCl

• Molecular Weight：192.26 (free base) + 2×36.46 (hydrochloride)

Applications

• Quality Control Testing：Used for UPLC-MS/MS detection of Impurity 84 in Rimegepant API and formulations, controlling content to meet ICH Q3A standards (single impurity limit ≤0.1%).

• Process Optimization Research：Monitors Impurity 84 formation during Rimegepant synthesis, reducing generation by >40% by adjusting condensation temperature (e.g., 60-70℃) and pH.

• Method Validation：Serves as a standard for developing impurity detection methods, verifying UPLC resolution (≥3.0) and LOD (0.01 ng/mL).

Background Description

Rimegepant, a CGRP receptor antagonist, is used for treating migraines. Impurity 84, as a process-related impurity, may originate from side products of amination between pyridine and piperidine during synthesis. Its amino and hydrochloride groups may affect drug stability and pH, requiring strict control for formulation safety. With stricter FDA requirements for migraine drug impurities, studying Impurity 84 is crucial for quality control.

Research Status

• Detection Technology：UPLC-MS/MS with C18 column (1.7μm) and 0.1% formic acid-acetonitrile gradient elution achieves separation within 6 minutes, with LOD of 0.005 ng/mL for trace impurity analysis.

• Formation Mechanism：Formed by condensation of 2,3-diaminopyridine with 4-chloropiperidine under alkaline conditions (e.g., triethylamine/DMF system) to give the free base, followed by salification with hydrochloric acid. Optimizing reaction time and hydrochloric acid dosage inhibits side reactions.

• Safety Evaluation：In vitro cytotoxicity shows IC?? of 185.3 μM against HEK293 cells (Rimegepant IC??=8.7 μM), with lower toxicity than the main drug but requiring strict content control. Long-term stability testing is ongoing to monitor degradation under different humidity and light conditions.