method for preparing a medicine containing a substituted thiophene derivative of pyrido - or pyridofuran is included.according to this method, the obtained product and process for the preparation of these active compounds.

摘要

1509256 Furo- and thieno[3,2-C]pyridines SANDOZ Ltd 22 Aug 1975 [27 Aug 1974 8 April 1975] 34917/75 Heading C2C The invention comprises compounds of Formula (I) and their acid addition salts, wherein X is S or O; R is C 3-7 alkyl or cycloalkyl, C 1-4 alkyl- C 3-7 - cycloalkyl, C 5-9 alpha - dialkyl - (allyl or propinyl), C 2-7 hydroxyalkyl or C 8-11 phenoxyalkyl (in the last two, the O is separated from N by at least C 2 ); R 1 is H, alkyl, 2-, 3- or 7-Cl, Br, NO 2 or NH(C 1-4 alkanoyl), or 2- or 3- F, CN or CO 2 (C 1-4 alkyl); and R 2 is H, alkyl, 2-, 3- or 7-Cl or Br, or 2- or 3-F. These compounds are prepared by (1) hydrolysing the oxazolidine derivative of Formula (II) in which CZZSP1/SP is a hydrolysable group, e.g. PhCH, or (2) reacting with the alkanolamine RNHCH 2 CHOHCH 2 OH a 4-chloro compound of Formula (III) where W is Cl or other anionic leaving group. Starting materials and intermediates otherwise prepared are 3-(2-methylthien-5-yl)acrylic acid, acid chloride and azide; 5-hydroxymethyl-2- phenyl-3-tert-butyloxazolidine; and some analogues of (III) in which W is OH. Therapeutic compositions which inhibit increased free fatty acid concentration in the blood and hyperglycaemia, induced by emotional stress, and which with certain exceptions possess also antiarrhythmic activity, comprise compounds of Formula (I)