摘要 |
Prepn. of cpds. - (I) R = alkyl opt. subst. by trihalomethyl, (5-6C) cycloalkyl, - where X1 = H, Hal, or alkyl, and a = 1-5 - R1 = H or alkyl - X = H, alkyl, or halogen, or 2 X's on adjacent C atoms = - CH=CH-CH=CH- - m = 1-4, n = 1-4 - R2 = H or alkyl, and R3 = aminoalkyl, pyrimidinyl, pyridyl, CO2 alkyl, laevo-alkaninyl, OH, CONH2, D-glucopyranosyl, polyhydroxyalkyl, or SO2 alkyl, or R2R3N = - Diuretics and saluretics. - (2,3-Dichloro-4-(2-methylenebutyryl) phenoxy) acetic acid (6.06g), SOCl2 (4.76g.), and PhH (15 ml.), were refluxed 1 1/4 h., and evapd. in vac.The residue was dissolved in PhH, 1-methylpiperazine (4.01g.) in PhH (25 ml.) added (1 1/4 h.), stirred 15 mins. at 20 deg., filtered, dild. with Et2O (50 ml.) and H2O (25 ml.) and sepd. The organic phase was washed with NaHCO3 and H2O, dried, evapd., and the residue (7.2g., m.p. 72-93 deg.) recryst. from cyclohexane, giving I (4.3g., 56%), m.p. 105-107 deg.
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