Felodipine

Base Information

• Chemical Name: Felodipine
• CAS No.: 72509-76-3
• Deprecated CAS: 86189-69-7
• Molecular Formula: C18H19Cl2NO4
• Molecular Weight: 384.259
• Hs Code.: 29333990
• European Community (EC) Number: 620-472-7
• NSC Number: 760343
• UNII: OL961R6O2C
• DSSTox Substance ID: DTXSID4023042
• Nikkaji Number: J11.263A
• Wikipedia: Felodipine
• Wikidata: Q420644
• NCI Thesaurus Code: C29046
• RXCUI: 4316
• Pharos Ligand ID: ZNJM1AZL7TDK
• Metabolomics Workbench ID: 43266
• ChEMBL ID: CHEMBL1480,CHEMBL3196476
• Mol file: 72509-76-3.mol

Synonyms:Agon;Felo Biochemie;Felo Puren;Felo-Puren;Felobeta;Felocor;Felodipin 1A Pharma;Felodipin AbZ;Felodipin AL;Felodipin AZU;Felodipin dura;Felodipin Heumann;Felodipin ratiopharm;Felodipin Stada;felodipin von ct;Felodipin-ratiopharm;Felodipine;Felodur;Felogamma;Fensel;Flodil;H 154 82;H 154-82;H 15482;Heumann, Felodipin;Modip;Munobal;Perfudal;Plendil;Renedil;Von Ct, Felodipin

Chemical Property of Felodipine

Chemical Property:

• Appearance/Colour: White or light yellow crystalline powder
• Vapor Pressure: 4.62E-09mmHg at 25°C
• Melting Point: 142-145 °C
• Refractive Index: 1.549
• Boiling Point: 471.5 °C at 760 mmHg
• PKA: 2.73±0.70(Predicted)
• Flash Point: 239 °C
• PSA: 64.63000
• Density: 1.277 g/cm³
• LogP: 4.29310
• Storage Temp.: Store at +4°C
• Solubility.: DMSO: 28 mg/mL
• Water Solubility.: insoluble
• XLogP3: 3.9
• Hydrogen Bond Donor Count: 1
• Hydrogen Bond Acceptor Count: 5
• Rotatable Bond Count: 6
• Exact Mass: 383.0691135
• Heavy Atom Count: 25
• Complexity: 614

Purity/Quality:

99% ^*data from raw suppliers

Felodipine ^*data from reagent suppliers

Safty Information:

• Pictogram(s): Xn
• Hazard Codes: Xn
• Statements: 22
• Safety Statements: 36

MSDS Files:

SDS file from LookChem

Total 1 MSDS from other Authors

Useful:

• Canonical SMILES: CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C
• Recent ClinicalTrials: Coffee Interaction With the Antihypertensive Drug Felodipine
• Recent EU Clinical Trials: An open-label, multicenter study to evaluate the efficacy and tolerability of a 4 week therapy with the combination of valsartan 160 mg plus amlodipine 5 mg in hypertensive patients not adequately responding to a 4 week treatment with amlodipine 5 mg or felodipine 5 mg in monotherapy
• Description: Felodipine is a vasodilatory calcium antagonist with a high degree of vascular selectivity. It is currently indicated for use only in hypertension, either as monotherapy or in conjunction with diuretics or beta blockers.
• Uses: vasodilator, Ca channel blocker Zanarnivir influenza prophylaxis and therapy Felodipine is used as a dihydropyridine calcium channel blocker. It displays high vascular selectivity; lowers arterial blood pressure without altering cardiac contractility. Antihypertensive.
• Therapeutic Function: Antihypertensive
• Clinical Use: Felodipine is used inthe treatment of angina and mild-to-moderate essential hypertension.Felodipine, like most of the dihydropyridines,exhibits a high degree of protein binding and has a half-liferanging from 10 to 18 hours.

Technology Process of Felodipine

There total 19 articles about Felodipine which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 99.3%

→ ethyl methyl 1,4-dihydro-2,6-dimethyl-4(2,3-dichlorophenyl)-3,5-pyridinedicarboxylate (72509-76-3,86189-69-7)

Guidance literature:

Reference yield: 96.0%

2-<(2,3-dichlorophenyl)methylene>-3-oxobutanoic acid ethyl ester (68064-64-2,94739-24-9,68064-63-1) + methyl 3-aminocrotonate (21731-17-9) → ethyl methyl 1,4-dihydro-2,6-dimethyl-4(2,3-dichlorophenyl)-3,5-pyridinedicarboxylate (72509-76-3,86189-69-7)

Guidance literature:

In ethanol; for 0.075h; Irradiation; Teflon vessel, microwave oven;

DOI:10.1055/s-1995-3933

Reference yield: 94.3%

ethyl 3-aminobut-2-enoate (626-34-6) + acetoacetic acid methyl ester (105-45-3) + 2,3-dichlorobenzylaldehyde (6334-18-5) → ethyl methyl 1,4-dihydro-2,6-dimethyl-4(2,3-dichlorophenyl)-3,5-pyridinedicarboxylate (72509-76-3,86189-69-7)

Guidance literature:

ethyl 3-aminobut-2-enoate; acetoacetic acid methyl ester; 2,3-dichlorobenzylaldehyde; With piperidine; pyridine; In neat (no solvent); at 75 - 80 ℃; for 9h;

With ethanol; for 1h; Reagent/catalyst; Solvent; Reflux;

upstream raw materials:

2-<(2,3-dichlorophenyl)methylene>-3-oxobutanoic acid ethyl ester

methyl 3-aminocrotonate

methyl iodide

1,1,1-Triphenyl-3-methyl-4-(methoxycarbonyl)-2-aza-1λ⁵-phosphabuta-1,3-diene

Downstream raw materials:

(R)-Felodipine

(S)-Felodipine

Dehydrofelodipine

Refernces

Asymmetric 4-Aryl-1,4-dihydropyridines Potentiate Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR)

10.1002/cmdc.201200311

The study focuses on the synthesis and evaluation of asymmetric 4-aryl-1,4-dihydropyridines (DHPs) as potential potentiators of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR), which is a protein affected by mutations causing cystic fibrosis (CF). The researchers synthesized a set of asymmetric DHPs and tested them on cells expressing different CFTR mutations, including G1349D, DF508, and G551D. The study aimed to identify compounds that could improve the function of the CFTR protein, particularly for class III mutations that impair channel gating. The most active racemates were then subjected to chiral separation to assess if a single enantiomer was responsible for the observed activity. The results showed that several DHPs had potentiating effects at nanomolar concentrations, but the chiral separation did not reveal significant differences in potency between the individual enantiomers, suggesting that the asymmetric nature of the DHPs was not critical for their activity as CFTR potentiators.

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