| 摘要 |
<p>Phthalimidine derivs. of general formula (I) R1 = H, 1-6C alkyl/alkenyl opt. substd. by OH or SH, free or esterified or etherified, amino, COOH, halogen; aralkyl, cycloalkyl or aryl opt. substd. m, n = 0-2 m+n = 1 or 2 As tumour-inhibitors and immunosuppressants. (a) A soln. of alpha-phthalimidoglutaric acid (133 g) in AcOH (1.2 l) at 60 deg. is treated gradually with Zn dust (168 g.) and the mixt. then refluxed for 4 hrs. to give alpha-phthalmidinoglutaric acid (70%), m.p. 236-7 deg. (water). (b) this (108 g), Ac2O (833 ml) and SOCl2 (29.7 ml) are refluxed to give the anhydride (90%). m.p. 254-7 deg. dec. (c) this (2.45 g.) and urea (0.3 g) are heated at 180 deg. for 90 mins. to give 3-phthalimidinopiperidine-2,6-dione, m.p.240-2.5 deg. (AcOH).</p> |
