Retrofits on or relating to new o - (2 - guanidino - ethyl) oxinas

摘要

1,144,875. Guanidine derivatives. PHILIPS' GLOEILAMPENFABRIEKEN N.V. 7 March, 1966 [10 March, 1965], No. 9888/66. Heading C2C. The invention comprises compounds of formula wherein R 1 and R 2 are hydrogen atoms or C 1-12 alkyl, aryl, aryloxyalkyl or aralkyl groups, which may be substituted by one or more halogen atoms or alkyl or alkoxy groups, or R 1 and R 2 together with the carbon atom to which they are attached form a C 4-14 saturated or unsaturated alicyclic group which may be substituted by one or more alkyl or aryl groups and/or may have one or two further alicyclic or aromatic rings condensed therewith, acid addition salts thereof, and their preparation by (a) reaction of a compound of formula or an acid addition salt thereof with cyanamide or with a compound of formula wherein X is a group easily replaced by an amino group, (b) reaction of a compound of formula R 1 R 2 C=NOH or a salt thereof with a compound of formula wherein X is a reactive ester group, (c) reaction of a compound of formula wherein Y is a halogen atom or a tosyloxy group, with guanidine or (d) reaction of a compound of formula R 1 COR 2 with 0-(2-guanidinoethyl)-hydroxylamine. Compounds of formula are prepared by reaction of a compound of formula R 1 R 2 C=NOH with aziridine or with a 2-halo- or 2-tosyloxy-ethylamine. The compounds of the invention have antihypertensive activity and may be used in pharmaceutical compositions in combination with a carrier for example in forms suitable for oral, parenteral or rectal administration.