Substituted thienylethylamines and process for their production

Details Substituted thienylethylamines and process for their production Substituted thienylethylamines and process for their production

1990-01-24

1991-01-08

Siegel, Alan

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

549 76, 549 77, C07D33312, C07D33322

Patent

active

049837443

ABSTRACT:
Substituted thienylethylamines of the formula: ##STR1## 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, are initial products for the production of antithromobolytically effective pharmaceutical agents. A process for the production of the above-mentioned compounds from substituted ethanolamines by their reaction with strong bases, further reaction with the resultant aziridines with 2-thienyllithium, and conversion of the resultant thienylethylamines with compounds of formula RX, wherein R has the above-mentioned meaning and X is a halogen.

REFERENCES:
patent: 4051141 (1977-09-01), Castaigne
patent: 4127580 (1978-11-01), Braye
patent: 4870076 (1989-09-01), Heckel et al.
The Merck Index, 10th Ed., (1983), p. 9274.
E. Saltiel et al., Drugs, 34, (1987), pp. 222-262.

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