ニフルジド

ニフルジド 化学特性,用途語,生産方法

• 効能

  止瀉薬, 抗感染症薬

• Originator

  Ricridene,Anphar,Switz.,1981

• Manufacturing Process

  (a) Ethyl-5-nitro-2-thiophene carboxylate:
  17.4 g (mol/10 = 17.31 g) of 5-nitrothiophene carboxylic acid are dissolved in 85 ml of absolute ethanol. A stream of gaseous hydrochloric acid is caused to enter the boiling solution to the point of saturation, and for 5 hours. Evaporation to dryness takes place and then the solid residue is washed with a sodium bicarbonate solution. It is suction-filtered and washed with water. After drying, there are obtained 17.7 g of a yellow product with a melting point of 63°C to 65°C and the yield is 88% (theoretical yield = 88%).
  The N'-(5'-nitro-2'-thenoyl)hydrazide is prepared by reacting hydrazine with ethyl 5-nitro-2-thiophene carboxylate.
  (b) 6.3 g (mol/30 = 6.5 g) of N1-[5'-nitro-2'-thenoyl]hydrazide are dissolved in 100 ml of dry tetrahydrofuran. 5.6 g (mol/30 = 5.55 g) of 5-nitro-2-furyl acrolein in 56 ml of tetrahydrofuran are added. Heating under reflux takes place for 1 hour and, 25 minutes after starting the heating, the crystallization commences; the crystals are suction-filtered, washed with ether and dried. There are obtained 7.9 g (yield 70%-theoretical yield = 11.2 g) of a yellow solid of melting point 235°C to 236°C.
  Recrystallization (tepid dimethylformamide + ether) leaves the melting point unchanged.

• Therapeutic Function

  Antibacterial, Antidiarrheal

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