process for the production of new pharmaceutical allowed saureadditionssalzen 1.1, dialkyl - n - butylaminen

摘要

1467740 1,1-Dialkyl-n-butylamines LABAZ 15 May 1975 [20 May 1974] 28336/76 Divided out of 1467739 Heading C2C Novel 1,1-dialkyl-n-butylamines of the general formula wherein R 1 is an ethyl or n-propyl group and R 2 is (a) an ethyl, isopropyl, isobutyl or tert. butyl group when R 1 is a n-propyl group and (b) a n-butyl or isobutyl group when R 1 is an ethyl group, and pharmaceutically acceptable acid addition salts thereof are prepared by treating an isocyanate of formamide of the general formula wherein A is -N=C=O or -NHCHO, with a strong acid in an appropriate medium, optionally treating the resulting acid addition salt with a base and optionally reacting the resulting free base with an acid to form a pharmaceutically acceptable salt. Novel 1,1 - di - n - propyl - n - butylamine acid fumarate is prepared by reacting the corresponding amine (1 mole) with fumaric acid (1 mole), the amine being prepared analogously to the amines (I). Isooyanates (II) are prepared by reacting an amide of the general formula with chlorine or bromine in an alkaline medium. 1,1 - Di - n - propyl - n - butyl isocyanate is prepared analogously. Formamides (II) are prepared by heating an alcohol of the general formula with an alkali metal cyanide in the presence of an acid. Alcohols (IV) are prepared by reacting an alkyl lithium with an appropriate dialkyl ketone in an anhydrous ether medium. Acids of the general formula are prepared by treating an alcohol (IV) with formic acid in a sulphuric acid medium.