摘要 |
Derivs. are of formula (I), in which R1 is CHO, CH2OH, CH2O-1-4C alkyl, CO-1-3C alkyl, CH(OH)-1-3C alkyl, or COOH; R2 is 1-4C alkyl, CHO, CH2OH, CH2O-1-4C alkyl, CO-1-3C alkyl, CH(OH)-1-3C alkyl, or COOH; R3 is 1-4C alkyl and X is pyrrolidinyl or pyrrolidinyl-methyl. They act on the central nervous system, blocking post-synaptic dopamine receptors in treatment of vomiting, depression, anxiety and certain psychotic conditions, and are made by (a) oxidn. of a cpd. (I) in which R1 or R2 is 1-4C alkyl or CHO; or (b) redn. of a cpd. (I) in which R1 or R2 is CHO or CO-1-3C alkyl, or (c) alkylation of a cpd. (I) in which R1 and/or R2 is CH2OH; or (d) reaction of a cpd. (II) in which Z is halogen, OH or OR and R is an active gp. with an amine of formula X-NH2.
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