Yamazaki H, Horikawa H, Nishitani T, Iwasaki T, Nosaka K, Tamaki H
Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1992 Jan;40(1):102-8. doi: 10.1248/cpb.40.102.
2,2,-Disubstituted norbornenes (1, 2), 2,2-Disubstituted norbornane (3), 2,2,3-trisubstituted norbornenes (4, 5), oxanorbornenes (6) and azanorbornenes (7) were synthesized by the Diels-Alder reaction using alpha, beta-dehydroamino acids as a key step, and their antiulcer activities were examined. The oxazolidine derivative (1h) exhibited the most potent activities against several ulcer-models in rat.
以α,β-脱氢氨基酸为关键步骤，通过狄尔斯-阿尔德反应合成了2,2-二取代降冰片烯（1, 2）、2,2-二取代降冰片烷（3）、2,2,3-三取代降冰片烯（4, 5）、氧杂降冰片烯（6）和氮杂降冰片烯（7），并检测了它们的抗溃疡活性。恶唑烷衍生物（1h）对大鼠的几种溃疡模型表现出最强的活性。
