Ethyl 1-aminocyclopropane-1-carboxylate hydrochloride → 4'-(4-chlorophenyl)-3'-methylspiro[cyclopropane-1,6'-isothiazolo[5,4-e][1,4]diazepin]-7'(8'H)-one

Participants

Reaction Conditions

Reaction Steps

A mixture of (5-amino-3-methylisothiazol-4-yl)(4-chlorophenyl)methanone (0.19 g, 0.75 mmol) and ethyl 1-aminocyclopropanecarboxylate hydrochloride (0.19 g, 1.13 mmol) in pyridine (1 mL) was heated at 170° C. for 18 h. The reaction mixture was then evaporated, extracted with water, dried over Na2SO4, filtered and evaporated. The crude product was purified by flash chromatography (EtOAc/hexane 0:10 to 5:5) to give 4′-(4-chlorophenyl)-3′-methylspiro[cyclopropane-1,6′-isothiazolo[5,4-e][1,4]diazepin]-7′(8′H)-one (35 mg).

Provenance & Evidence