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alpha-(1-Naphthylmethyl)-2-tetrahydrofuranpropionic acid diethylaminoethyl ester oxalate

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alpha-(1-Naphthylmethyl)-2-tetrahydrofuranpropionic acid diethylaminoethyl ester oxalate Basic information

Product Name:
alpha-(1-Naphthylmethyl)-2-tetrahydrofuranpropionic acid diethylaminoethyl ester oxalate
Synonyms:
  • 2-(diethylamino)ethyltetrahydro-alpha-(1-naphthylmethyl)-2-furanpropionateo
  • eu-1806
  • hylester,oxalate(1:1)
  • ls121
  • naftidrofuryloxalate
  • diethyl[2-[2-(1-naphthylmethyl)-3-(tetrahydro-2-furyl)propionyloxy]ethyl]ammonium hydrogen oxalate
  • CLARANTIN
  • Nafronyl acid oxalate
CAS:
3200-06-4
MF:
C26H35NO7
MW:
473.56
EINECS:
221-703-0
Product Categories:
  • CASODEX
Mol File:
3200-06-4.mol
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alpha-(1-Naphthylmethyl)-2-tetrahydrofuranpropionic acid diethylaminoethyl ester oxalate Chemical Properties

Melting point:
110-111°
Boiling point:
574°C (rough estimate)
Density 
1.2205 (rough estimate)
refractive index 
1.6000 (estimate)
storage temp. 
Store at -20°C
solubility 
Freely soluble in water, freely soluble or soluble in ethanol (96 per cent), slightly or sparingly soluble in acetone.
form 
Solid
color 
White to off-white
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Safety Information

Hazard Codes 
Xn,Xi
Risk Statements 
22
Safety Statements 
36
WGK Germany 
3
RTECS 
LU5805000
HS Code 
29321900
Toxicity
LD50 oral in rat: 711mg/kg

MSDS

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alpha-(1-Naphthylmethyl)-2-tetrahydrofuranpropionic acid diethylaminoethyl ester oxalate Usage And Synthesis

Chemical Properties

White solid

Originator

Dusodril,Roland,W. Germany,1968

Uses

antineoplastic

Manufacturing Process

30 grams (0.106 mol) of β-(1-naphthyl)-β'-tetrahydrofuryl isobutyric acid are heated under reflux for 8 1/2 hours in 230 cc of isopropanol with 14 grams (0.103 mol) of β-chloroethyl-N-diethylamine. After evaporation of the isopropanol in vacuo, the syrupy residue is treated with a solution of K2CO3. Extraction with ether is carried out after drying over Na2SO4.
Distillation of the extract yields 28.5 grams of a very viscous yellow liquid with a BP0.95-1.09millibar = 198° to 202°C. The yield is 70.5% (theoretical quantity = 40.5 grams).1.3 grams (0.0103 mol) of dihydrated oxalic acid are dissolved while being made tepid in 8 cc of acetone. The cooled solution has added thereto 4 grams (0.0104 mol) of N-diethylaminoethyl-β-(1-naphthyl)-β'- tetrahydrofuryl isobutyrate, obtained according to the process described above and dissolved in 10 cc of acetone. The solution is brought to boiling point for 15 minutes. After cooling to ambient temperature, it is placed in a refrigerator. Crystallization occurs after 2 hours, the crystals which have formed are separated by centrifuging, and after washing in hexane and drying in vacuo 3.5 grams of white crystals are obtained. After being recrystallized three times, in alcohol and then in a mixture of alcohol and ethyl acetate, the product is analytically pure and has a MP = 110° to 111°C (heating stage).

brand name

Praxilene (Lipha, S.A., France).

Therapeutic Function

Vasodilator

Clinical Use

Vasodilator:
Peripheral and cerebral vascular disease

Metabolism

Metabolised by plasma pseudo-cholinesterases to 3 active metabolites.

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