Claims
- 1. Process for the production of a substituted thienylethylamine of the formula: ##STR9## wherein R is formyl, acetyl or benzoyl or is benzyl, which is ring-substituted by at least one halogen atom, and R.sub.1 is lower alkyl, phenyl or substituted phenyl, comprising: converting a substituted ethanolamine of the formula: ##STR10## wherein R.sub.1 has the above-mentioned meaning, with a strong base to an aziridine of the formula: ##STR11## wherein R.sub.1 has the above-mentioned meaning, converting the aziridine of formula (II) with 2-thienyllithium to a thienylethylamine of the formula: ##STR12## wherein R.sub.1 has the above-mentioned meaning, and converting the thienylethylamine of formula (III) with a compound RX, wherein R has the above-mentioned meaning and X is chlorine, bromine or iodine, to the thienylethylamine of formula (IV).
- 2. Process according to claim 1 wherein an alkali hydride, alkali amide or alkyllithium is used as the strong base.
- 3. Process according claim, 1 or 2 wherein the conversion to the aziridine takes place at a temperature between -80 and +100.degree. C. in an inert solvent.
- 4. Process according to claim 1 wherein the reaction with 2-thienyllithium takes place at a temperature between -80.degree. and +60.degree. C. in an inert solvent.
- 5. Process according to claim 1 wherein the reaction with the compound RX takes place at a temperature between -50 .degree. and +100.degree. C.
- 6. Process according to claim 1 wherein the process takes place without isolation of the intermediate products.
Priority Claims (1)
Number |
Date |
Country |
Kind |
3795/88 |
Oct 1988 |
CHX |
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Parent Case Info
This is a divisional of application Ser. No. 418,340, of Aleksander WARM et al., filed on Oct. 6, 1989.
US Referenced Citations (3)
Non-Patent Literature Citations (2)
Entry |
The Merck Index, 10th Ed., (1983), p. 9274. |
E. Saltiel et al., Drugs, 34, (1987), pp. 222-262. |
Divisions (1)
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Number |
Date |
Country |
Parent |
07418340 |
Oct 1989 |
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