2426-86-0Relevant articles and documents
Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2
Groszek, Grazyna,Nowak-Krol, Agnieszka,Wdowik, Tomasz,Swierczynski, Dariusz,Bednarski, Marek,Otto, Monika,Walczak, Maria,Filipek, Barbara
experimental part, p. 5103 - 5111 (2010/02/28)
The synthesis of (2RS)-1-(5-methoxy-1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and (2RS)-1-(7-methoxy-1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and its enantiomers, analogs of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol ((RS)-9) is described. Compounds were tested for electrographic, antiarrhythmic, hypotensive and spasmolytic activities as well as for α1-, α2- and β1-adrenoceptors binding affinities. The antagonist potency of the new compounds was compared with carvedilol and (RS)-9.
Synthesis of 4-chloro-7-ethoxy-2(3H)-benzoxazolone-6-carboxylic acid
Kato, Shiro,Morie, Toshiya
, p. 1171 - 1178 (2007/10/03)
As a part of metabolic studies of mosapride (1), a potential gastroprokinetic agent, the synthesis of 4-chloro-7-ethoxy-2(3H)-benzoxazolone-6-carboxylic acid (7) as a derivative of 4-amino-5-chloro-2-ethoxy-3-hydroxybenzoic acid (6), which has served a benzoic acid part of the metabolites 4 and 5, is described. Treatment of methyl 3-amino-4-substituted amino-5-chloro-2-ethoxybenzoate derivatives 11a-c with sodium nitrate in acidic medium gave the benzotriazole derivatives 13x,y instead of the objective 3-hydroxy counterpart. The synthesis of 7 started from o-vanillin acetate (15) and proceeded through the intermediates 2-hydroxy-3-methoxy-4-nitrobenzaldehyde (18), methyl 4-amino-2,3-dihydroxybenzoate (23), and methyl 7-hydroxy-2(3H)-benzoxazolone-6-carboxylate (30). Compound 30 was alternatively prepared from 23 via methyl 4-ethoxycarbonylamino-2-ethoxycarbonyloxy-3-hydroxybenzoate (29), which is the product resulting from the migration of the ethoxycarbonyl group of methyl 4-amino-2,3-diethoxycarbonyloxybenzoate (27).
Substituted quinazolinediones
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, (2008/06/13)
The synthesis of 5,6-dioxy substituted quinazolinediones is described. The novel quinazolinediones are useful as cardiotonic agents.