Clevidipine butyrate

Clevidipine butyrate
  • CAS No.:167221-71-8
Other grades of this product :
Clevidipine butyrate Basic information
Product Name:Clevidipine butyrate
Synonyms:Methyl (1-oxobutoxy)methyl 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dime thyl-3,5-pyridinedicarboxylate;4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-Pyridinedicarboxylic acid methyl (1-oxobutoxy)methyl ester;3,5-Pyridinedicarboxylicacid, 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-, 3-methyl5-[(1-oxobutoxy)methyl] ester;Clevidipine butyrate;Cleviprex;Clevidipine, Cleviprex;CS-136;CLEVELOX; CLEVIDIPINE
CAS:167221-71-8
MF:C21H23Cl2NO6
MW:456.32
EINECS:682-702-2
Product Categories:Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Clevidipine Butyrate impurity;Cardiovascular APIs;API
Mol File:167221-71-8.mol
Clevidipine butyrate Chemical Properties
Melting point 128-130°C
Boiling point 539.7±50.0 °C(Predicted)
density 1.289
Fp 280℃
storage temp. Keep in dark place,Inert atmosphere,2-8°C
Water Solubility Insoluble in water
solubility ≥21.4 mg/mL in DMSO; insoluble in H2O; ≥7.45 mg/mL in EtOH with ultrasonic
form powder to crystal
pka2.45±0.70(Predicted)
color White to Light yellow
CAS DataBase Reference167221-71-8
Safety Information
Safety Statements 24/25
HS Code 29339900
MSDS Information
Clevidipine butyrate Usage And Synthesis
DescriptionClevidipine is an ultra-short-acting vasodilator of the dihydropyridine (DHP) class of CCB. It is indicated as an intravenous treatment for the acute management of hypertension when oral therapy is not feasible or not desirable. Clevidipine is the second intravenous CCB to be marketed behind nicardipine for this indication. Both agents are primarily used for urgent treatment of hypertension in cardiac surgical setting, intensive care units, and emergency departments. Other intravenous agents currently on the market for this indication include sodium nitroprusside, nitroglycerin, fenoldopam, hydralazine, esmolol, and labetalol. Clevidipine is a potent, arterial-specific, vasodilator with very little or no effect on the myocardial contractility and venous capacitance. It has a rapid onset and offset of action and a very short plasma half-life, which allows for titration of the drug to achieve precise BP control.clevidipine is exclusively metabolized in the blood and the tissues. It does not undergo any renal or hepatic metabolism and does not accumulate in the body. Clevidipine is a blocker of L-type calcium channels, which mediate the influx of calcium during depolarization in arterial smooth muscle.
Chemical PropertiesWhite to Off-White Solid
OriginatorAstraZeneca (United Kingdom)
UsesClevidipine butyrate is a dihydropyridine calcium channel blocker use as agent for the reduction of blood pressure。
UsesCalcium channel blocker, used as an oral antihypertensive.
UsesClevidipine butyrate is a novel intravenous, short-acting calcium channel blocker that provides quick and accurate control of blood pressure in an emergency setting. Unlike other intravenous hypertension drugs which are metabolized in kidney or liver and tend to accumulate in the body, clevidipine is metabolized in the blood and tissues and thus avoids accumulation. The drug was launched by Medicines Company which aquired the rights from AstraZeneca.
UsesA calcium channel protein inhibitor and blocker
Brand nameClevelox (The Medicines Company).
Side effectsClevidipine is contraindicated in patients with severe aortic stenosis, defective lipid metabolism, and allergies to eggs, egg products, soybeans, or soy products. The chemical synthesis of clevidipine entails the esterification of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid monomethyl ester with chloromethyl butyrate by the action of potassium bicarbonate in refluxing acetonitrile.
SynthesisThe chemical synthesis of clevidipine entails the esterification of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid monomethyl ester with chloromethyl butyrate by the action of potassium bicarbonate in refluxing acetonitrile. The DHP-monoester starting material is obtained in two steps through condensation of methyl 2,3-dichlorobenzylidine acetoacetate and 2-cyanoethyl ester of 2-amino-2-propenoic acid to the DHP diester, followed by base catalyzed cleavage of the cyanoethyl group. Clevidipine is practically insoluble in water and is formulated in an oil-inwater emulsion.
Clevidipine butyrate Preparation Products And Raw materials

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