N-(2,2,2-Trihalo-1-(thia)morpholino-ethyl)-carbamates or-formamides - prepd by reacting (thia)morpholines with N-(1,2,2,2-tetrahaloethyl) cpds

摘要

Carbamates or formamides of formula (I) (where R1 is H or 1-8C alkoxy; X1 is H, Cl or Br; X2 and X3 are Cl or Br; Y is O or S; R is 1-4C alkyl and/or phenyl; and n is 1,2 or 3; provided that when n is 2 the two R's are not both methyl or both phenyl, or the two R's are methyl in the 2,2-, 2,5- or 2,6-position), e.g. N-(1-formamido-2,2,2-trichloroethyl)-2,6-dimethylmorpholine or N-(1-ethoxycarbonylamino-2,2,2-trichloroethyl)-2,6-dimethylmorpho- line, and their pharmacologically tolerable salts are new cpds. (I) have sedative, hypnotic, narcotic and anticonvulsant activity and can be used e.g. in the treatment of sleep disorders; dosage is 100-200 mg. Results of pharmacological tests are given in the specification; thus, 4-(1-formamido-2,2,2-trichloroethyl)2-methyl-morpholine in a dosage of 46.4, 100 or 215mg/kg p. o gives a lowering of rat body temperature of 1.82, 2.00 or 3.07 degrees C, resp. (lowering of body temp. is a measure of sedative and narcotic activity).