摘要 |
(A) Cpds. of general formula (I) including all stereoisomers. - R' = alkyl or aryl - R2 and R3 = H, alkyl or aryl - R4 = OH, an ether, or an ester gp. - and X and Z = H, OH, alkyl, O-alkyl, hal, or haloalkyl - (B) Salts of I - C.N.S. stimulants and anorexics (if R4 = OH or Oacyl). - D-alpha-methylphenylethylamine (55.0 g.) and epichlorohydrin (36.6 g.), were stirred 24 h. at 25 deg. in Me2SO (92 g.), heated 7 d. at 45-50 deg., cooled, added 10% NaOH (200 ml) and extd. with Et2O (3x 100 ml). The Et2O was washed with H2O (3x100 ml), evapd., and distilled, giving D-1-(alpha-methylphenylethyl) -3-azetidinol (16 g.), b.p. 118-121 deg./0.1 mm., m.p.105-105.5 (from hexane).
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