3-isocyanothiophenes antibacterial and antifungal

摘要

New cpds. of formula: (R1 = H, alkyl (C1-C6), alkoxycarbonyl (C2-C5), CN, phenyl; R2 = H, alkyl or alkoxy (C1-C6), alkoxycarbonyl (C2-C5), CN, phenyl; R3 = H, alkyl (C1-C6), alkoxycarbonyl (C2-C5), phenyl; R2 and R3 together may form an alkylene chain (C3-C4) to complete a fused ring). - Used as antibacterial and antifungal agents for topical application e.g. against Trichophyton, Microsporum, Epidermophyton, Candida albricans. Applied in conventional formulations containing 0.25-10% of (I) on the skin and 0.25-0.5% of (I) on mucosa. - Preparation is as follows: (a) - H2X right arrow (I) (X = O or S) (b) + CHCl3 strong base right arrow (I) (c) Reduction of 3-isocyanates (d) Treatment of 3-isothiocyanates with tert. phospines (e) Dehalogenation of 3-isocyano-dihalides.