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| | ETILEFRINE-D5 Basic information |
| | ETILEFRINE-D5 Chemical Properties |
| Melting point | 147-148° | | Boiling point | 314.35°C (rough estimate) | | density | 1.0918 (rough estimate) | | refractive index | 1.5464 (estimate) | | pka | 9.81±0.10(Predicted) | | LogP | 3.2 at 25℃ and pH5.5 |
| | ETILEFRINE-D5 Usage And Synthesis |
| Originator | Circupon,Troponwerke,W. Germany | | Uses | Etilefrin is a sympathomimetic drug that increases the pulse rate, cardiac output, stroke volume, central venous pressure and mean arterial pressure of healthy individuals. Etilefrin has both beta 1 and alpha adrenergic effects on humans and is mainly used for the treatment of patients with orthostatic hypotension. | | Uses | ETILEFRINE-D5 is a sympathomimetic drug that increases the pulse rate, cardiac output, stroke volume, central venous pressure and mean arterial pressure of healthy individuals. Etilefrin has both beta 1 and alpha adrenergic effects on humans and is mainly used for the treatment of patients with orthostatic hypotension. | | Definition | ChEBI: 3-[2-(ethylamino)-1-hydroxyethyl]phenol is a member of phenols. | | Manufacturing Process | 30 parts of 1-(3'-hydroxyphenyl)-2-(N-benzylaminomethyl)-ethan-1-one are
mixed with 100 parts of pyridine and 30 parts of pivalic anhydride and
dissolved while warming. After heating for 1 hour under reflux, the acylation
is complete. After concentrating the reaction solution, the product is
precipitated from acetone/ether. Yield: 96.4% of 1-(3'-pivaloyloxyphenyl)-2-
(N-benzylaminomethyl)-ethan-1-one.
3 parts of palladium/charcoal (10% strength) are prehydrogenated in water,
thereafter 10 parts of 1-(3'-pivaloyloxyphenyl)-2-(N-benzylaminoethyl)-ethan-
1-one, dissolved in a 10-fold amount of water, are added dropwise at room
temperature and hydrogenation is carried out until 1 mol of hydrogen has
been taken up. After filtering off the catalyst, a further 3 parts of
palladium/charcoal are added and hydrogenation is carried out until a further
mol of hydrogen has been taken up. The catalyst is separated off and after
removal of the solvent the hydrogenation product is reprecipitated from
acetone/petroleum ether and from methanol/ether until it is pure according to
thin layer chromatography. Yield: 38.8% of 1-(3'-pivaloyloxyphenyl)-2-
ethylaminoethanol-1 hydroxide, melting point 208°C to 209°C. | | Therapeutic Function | Tranquilizer |
| | ETILEFRINE-D5 Preparation Products And Raw materials |
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