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CAS No.130929-57-6 | Entacapone

Name:Entacapone CAS No.130929-57-6 MF:C14H15N3O5 MW:305.29 Purity:97% Package: 10g,25g,50g,100g,250g Worldwide Delivery

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Biochemicals

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Product introduction

Introduction and application of CAS No.130929-57-6 | Entacapone

Specification:

ITEMS	SPECIFICATION
CAS	130929-57-6
MF	C14H15N3O5
MW	305.29
Melting point	162-1630C
Boiling point	526.6±50.0 °C
Density	1.392±0.06 g/cm
Acidity coefficient	pKa ~4.5(at 25℃)
Color	white to light brown
Solubility	Solubility in DMSO is 20mg/mL, clear
Form	Powder
Storage condition	2-8°C

Production method:

Dissolve 1.83g of 3,4-dihydroxy-5-nitrobenzaldehyde, 1.5g of N,N-diethylcyanoacetamide and a catalytic amount of piperidine acetate in 40ml of dry ethanol, and stir overnight to obtain 2.23 g crude product, yield 73%, melting point 153~156°C. Heating at 90°C, dissolve 3.0kg of crude product in 8.0kg of acetic acid (or formic acid) containing 80gHBr (or 40gHCl). Cool slowly to 20°C and stir at this temperature for 20h, then at 15°C for 6h. Collect the precipitated crystals by filtration, first carefully wash them with cold (4°C) 1L toluene-acetic acid (1:lv/v) mixture, and then wash them with 1L cold toluene. Dry under vacuum and 45°C to obtain 2.4kg of crystalline pure entacapone, with a yield of 80% and a melting point of 162--163°C.

Purpose; It is a COMT inhibitor, used to treat Parkinson's disease.

Entacapone is an anti-Parkinson's disease drug successfully developed by the Swedish company OrionPharma. It is a highly selective and potent catechol oxygen methyltransferase (COMT) inhibitor that rarely penetrates the blood-cerebrospinal fluid barrier. , mainly works in the intestines. Dose-related reductions in serum and brain 3-OMD levels, increases in brain levels of levodopa, dopamine, and DOPAC and significantly reduces the dose required to increase striatal dopamine concentrations. Combining levodopa and carbidopa with COMTI can significantly increase the bioavailability of levodopa (3 to 4 times). The activity of COMTI in red blood cells is reversible. At a dose of 800 mg, the maximum inhibitory activity can reach 82%. Therefore, entacapone combined with levodopa and carbidopa can be used for the adjuvant treatment of primary Parkinson's disease.

Package and transportation :

Package: 10g,25g,50g,100g,250g