(1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine (2R)-Hydroxy(phenyl)ethanoate

Product Name:(1R
2S)-2-(3
4-Difluorophenyl)cyclopropanamine (2R)-Hydroxy(phenyl)ethanoate
CAS:376608-71-8
MFC17H17F2NO3
MW:321.32
EINECS:1308068-626-2
MOL File:376608-71-8.mol

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Product Overview: (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine (2R)-Hydroxy(phenyl)ethanoate

Table of Contents

Parameter Value
CAS Number 376608-71-8
Molecular Formula C16H15F2NO3
Appearance Off-white to pale yellow crystalline powder
Purity ≥99% (HPLC)
Optical Purity ≥98% ee

Technical Specifications & Comparative Analysis

This chiral cyclopropane derivative serves as critical intermediate in antithrombotic drug synthesis. Structural analogs differ in stereochemistry at positions 1R/2S versus 1S/2R configurations, significantly impacting biological activity. The (2R)-hydroxy(phenyl)ethanoate counterion enhances stability during API manufacturing compared to hydrochloride salts.

Pharmaceutical Applications

Primary application: Key intermediate for Ticagrelor (Brilinta®), a P2Y12 platelet inhibitor. Required for constructing the cyclopropane-containing pharmacophore that enables irreversible binding to ADP receptors. Global demand driven by cardiovascular treatment markets, with annual consumption exceeding 8 metric tons.

Quality Control Parameters

Test Specification
Residual Solvents ≤500 ppm (ICH Q3C)
Heavy Metals ≤10 ppm (USP <232>)
Enantiomeric Excess ≥98% (Chiral HPLC)

Industrial Case Studies

Case 1: Jiangsu Pules Biotech (2024) achieved 92% yield improvement through asymmetric cyclopropanation optimization, reducing critical impurities to <0.1%.

Case 2: Wuhan Lihe Pharma’s continuous flow synthesis platform (2025 Q1) demonstrated 40% cost reduction while maintaining 99.5% chiral purity.

Procurement Guidance

  1. Verify chiral purity certificates with CDMO’s analytical reports
  2. Require ICH stability data (accelerated 40°C/75% RH)
  3. Confirm regulatory support for DMF/CEP filings

Supplier Inquiry

Contact our technical team for current batch availability and custom synthesis options:

Email: info@vivalr.com
Tel: (86) 15866781826

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