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Specifications
| Appearance | White to yellow powder |
| Chromatographic Purity | 99% min |
| Solubility | Practically insoluble in water, sparingly soluble in acetone and ethyl acetate |
| Identification | RT of sample to match with RS on HPLC Infrared spectrum corresponds to that of RS |
| Loss on drying | 0.5% max |
| Individual impurity | 0.1% max |
| Total impurities | 0.7% max |
| Impurity 2 | 0.1% max |
| Impurity 1 | 0.08% max |
Applications
Phthaloyl amlodipine (CAS 88150-62-3) is a derivative of amlodipine, a widely used calcium channel blocker, and is primarily utilized as an intermediate in pharmaceutical synthesis. It serves as a key building block in the preparation of amlodipine formulations and related analogs. In medicinal chemistry, phthaloyl amlodipine is employed to modify the amine functionality of amlodipine, allowing controlled release or improved stability in drug development. It is also used in structure–activity relationship (SAR) studies to optimize pharmacokinetic and pharmacodynamic properties of cardiovascular drugs, particularly for hypertension and angina treatment.
Benefits
The benefits of phthaloyl amlodipine are mainly related to its chemical protection and stability. The phthaloyl group protects the amine functionality during multi-step synthetic processes, preventing unwanted reactions and facilitating selective transformations. This allows for higher yields and purity in the synthesis of amlodipine and related compounds. Additionally, its stability under standard reaction conditions makes it a reliable intermediate in pharmaceutical manufacturing. The ability to selectively deprotect the phthaloyl group at later stages provides flexibility in designing drug molecules and derivatives with desired activity and solubility profiles.
Conclusion
Phthaloyl amlodipine is a valuable pharmaceutical intermediate that enables efficient synthesis and modification of amlodipine and related calcium channel blockers. Its protective phthaloyl group ensures chemical stability and selectivity during synthesis, supporting high-quality production and structural optimization of cardiovascular drugs. By combining stability, reactivity, and synthetic versatility, it continues to play a critical role in medicinal chemistry and pharmaceutical development.

