Process for the preparation of 3,4-bis-substituted 1,...

Details Process for the preparation of 3,4-bis-substituted 1,... Process for the preparation of 3,4-bis-substituted 1,...

C - Chemistry, Metallurgy

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C07D 413/14 (2006.01) A61K 31/42 (2006.01) A61K 31/475 (2006.01) A61K 31/50 (2006.01) A61K 31/505 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) C07D 271/08 (2006.01) C07D 295/18 (2006.01)

Patent

CA 1157019

ASTRACT Process for the preparation of pharmacolically valuable 3,4-bis-substituted 1,2,5-oxdiazole 2-oxides of the formula I (1) Image and their pharmacologically acceptable acid addition compounds, wherein R denotes -NHR1, -NR2R3, -NHR4OR2, -NHR5COR6 or Image R1 denotes alkyl having 1 to 6 C atoms or cycloalkyl having 4 to 7 C atoms, R2 and R3 denote alkyl having 1 to 4 C atoms, R4 denotes an alkylene radical of the formula -CnH2n- wherein n denotes 2, 3 or 4, R5 denotes an alkylene radical of the formula -CmH2m- wherein m denotes 1, 2 or 3, R6 denotes -OR2,-NHR1,-NR2R3 or -NH2, X denotes -(CH2)p-, Image and p is 4, 5 or 6, by elimination of hydrogen chloride from a hydrox- amoyl chloride of the formula II Image (II) and dimerisation and also, if desired, subsequent conversion into the acid addition compound,

392512

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