Disclosed is a novel arylalkylamine derivative represented by the formula (I) ##STR1## wherein X represents --O--, --CH.sub.2 -- or --NR.sup.3 -- in which R.sup.3 represents hydrogen or lower alkyl; Y represents --NH-- or ##STR2## Z represents ##STR3## in which R.sup.4 represents hydrogen or lower alkyl or ##STR4## Q represents an optionally substituted aryl or optionally substituted aromatic heterocyclic group; each of R.sup.1 and R.sup.2 independently represents hydrogen or lower alkyl; each of m and n independently represents an integer of 0 or 1; and a pharmaceutically acceptable salt thereof. The compound (I) and a pharmaceutically acceptable salt thereof show bronchodilatory and antiallergic activities, and are useful for treating respiratory disorders such as bronchial asthma.
Process for the preparation of arylalkylamines and substituted arylalkylamines
申请人:HOECHST CELANESE CORPORATION
公开号:EP0491557A1
公开(公告)日:1992-06-24
Arylalkylamines (as the hydrochloride salt), e.g. tyramine hydrochloride, are prepared by hydrogenating substituted or unsubstituted aryl-α-oximinoalkyl ketones, e.g. p-hydroxyisonitroacetophenone, in either in an aqueous reaction medium comprising hydrochloric acid, essentially without the presence of a lower alkyl alcohol in said reaction medium, or in an aqueous reaction medium comprising water, hydrochloric acid, and a lower alkyl alcohol, wherein the alcohol comprises less than about 90% by volume of the reaction medium. A substituent on the aryl portion of the aryl-α-oximinoalkyl ketone must be on a position which activates the aromatic ring.
Quantitative measurement of octopamines and synephrines in urine using capillary column gas chromatography negative ion chemical ionization mass spectrometry
作者:Kamal E. Ibrahim、Margaret W. Couch、Clyde M. Williams、Mary Beth. Budd、Richard A. Yost、John M. Midgley