| 摘要 |
<p>(A) Indole derivs. of the general formula: (I) where R1 and R2 = H or alkyl; R5 = H, alkyl, aralkyl, or acyl; n = 0-4; Y = NHNHR4; R4 = H, acyl, or carbalkoxy; Z = CN, CONH2, or CO2R3; R3 = H or alkyl; or Y and Z together are=NNHR4. (B) Salts of I. (a) I where Y = NHNHR4 and Z = CO2R3, are anti-inflammatories. Dose 10-350 mg/day. (b) Remainder are intermediates for (a). beta-(Indolyl-(3))-alpha-sulphhydrylacrylic acid (1.97 g), MeOH (7 ml), and N2H4.H2O (2.40 ml), were refluxed 2 h. under N2, filtered, washed (EtOH), and vac.-dried at 50 deg.C., giving (indolyl-(3)) pyruvic acid hydrazone N2H4 m.p. 156 deg.C. This (33.0 g), in H2O (300 ml), was treated with 2.3% Na-Hg (92.0 g), (added over 1 hr.), stirred 80 h. at 25 deg.C., aqueous phase decanted, decolourised (3.0 g charcoal), filtered, acidified to pH 5.5 (HOAc), filtered, and washed. Solid suspended in H2O (200 ml), acidified (50% HCl) to pH 1.2, filtered, and added NaOAc (15 g) in H2O (40 ml), giving a ppt. of alpha-hydrazino-beta-(indolyl-(3))-propionic acid m.p. 260 deg.C.</p> |
