abstract |
1,247,306. Isoquinoline and 3-benzazepin compounds from glyoxylic acid. LABORATOIRES HOUDE. 20 Aug., 1969 [2 Sept., 1968], No. 41485/69. Heading C2C. The invention comprises compounds of formula wherein R and R<SP>1</SP> are each H or C 1-5 alkyl and R<SP>11</SP> is H or OH, and a method of making them by reacting 1 mole of with 1 mole of (HO) 2 CHCO 2 R<SP>1</SP>. The isoquinaldic acid esters may be hydrolysed (e.g. with NaOH) to the acids, and the reverse may be effected using e.g. R<SP>1</SP>OH + HC1; the acid where R = H may be methylated with formic acid + formalin. Cis and trans forms of the acids are prepared. Therapeutic compositions for oral and rectal administration comprise compounds of the above formulĀµ, which have anti-tussive activity. |