톨시클레이트

톨시클레이트 화학적 특성, 용도, 생산

• Originator

  Tolmicen,Carlo Erba,Italy,1979

• Manufacturing Process

  Thiophosgene (1.15 g, 0.01 mol) in chloroform (40 ml) was slowly treated at room temperature with sodium 1,4-methano-1,2,3,4-tetrahydro-6- naphthoxide (1.82 g, 0.01 mol). After 30 minutes, N-methyl-m-toluidine (2.42 g, 0.02 mol) in chloroform (40 ml) was added dropwise to the solution so obtained at room temperature. The reaction mixture was stirred for 48 hours at room temperature and then refluxed for 2 hours. The solvent was evaporated, and the residue redissolved in water and extracted repeatedly with diethyl ether. The organic phase was dried (Na2SO4) and evaporated to dryness to give, after crystallization from isopropanol, O-(1,4-methano- 1,2,3,4-tetrahydro-6-naphthyl)-N-methyl-N-(m-tolyl)-thiocarbamate (1.3 g) melting point 92°C to 94°C.

• Therapeutic Function

  Topical antimycotic

• Antimicrobial activity

  In vitro, tolciclate has a narrow activity spectrum with good efficacy only towards dermatophytes. Isolates of susceptible species showing primary resistance or developing secondary resistance are rarely observed.

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