Process for the preparation of 4-amino-6-tert.-butyl-...

Details Process for the preparation of 4-amino-6-tert.-butyl-... Process for the preparation of 4-amino-6-tert.-butyl-...

C - Chemistry, Metallurgy

07

D

260/248.6

C07D 253/06 (2006.01) C07C 51/06 (2006.01) C07D 253/075 (2006.01)

Patent

CA 1148543

ABSTRACT In the preparation of 4-amino-6-tert.-butyl-3-alkylthio- 1,2,4-triazin-5-(4H)-one of the formula Image wherein (1) pivaloyl cyanide of the formula (CH3)3C-CO_CN is reacted to form a derivative of pyruvic acid, (2) the pyruvic acid derivative is condensed with thiocarbohydrazide of the formula NH2_NH-CS-NH-NH2 to form 4-amino-6-tert.-butyl-3-mercapto-1,2,4-triazin-5(4H)- one of the formula Image and (3) this is alkylated, the improvement which comprises effecting step (1) by reaction with a carboxylic acid anhydride of the formula R-CO-O-CO-R in which R is an optionally substituted aliphatic radical with up to 8 carbon atoms or an optionally substituted phenyl radical, in the presence of a strong acid at a temperature between about -50 and +150°C, and then adding water to the reaction mixture, thereby to form trimethylpyruvic acid N-acylamide of the formula (CH3)3C-CO-CO-NH-CO-R.

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