PURPOSE: To obtain a compound useful as a synthetic intermediate for medicines in high yield without isolating intermediate products by passing a toluene compound as a starting substance through a dihalogenomethylbenzene and diazidomethylbenzene.
CONSTITUTION: A toluene compound expressed by formula I (R1 and R2 are H, halogen, nitro or alkoxy) is reacted with N-bromosuccinimide or N- chlorosuccinimide in an inert solvent (e.g. carbon tetrachloride) to provide a dihalogenomethylbenzene compound expressed by formula II (X1 and X2 are Br or Cl), which is then reacted with an alkali metallic azide, an alkaline earth metallic azide or ammonium azide in an inert solvent (e.g. N,N- dimethylformamide) to afford a diazidomethylbenzene compound expressed by formula III. Thermal decomposing reaction of the resultant compound is subsequently carried out at 50-200°C in an inert solvent (e.g. the N,N- dimethylformamide) to provide the objective 5-aryl-1H-tetrazole compound expressed by formula IV.
USUI TOSHINAO
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