Synthesis of cis-bicyclo(4.3.0)non-2-ene derivatives. The potent homoisocarbacyclin analogs.
作者:Masakatsu SHIBASAKI、Atsuo TAKAHASHI、Tsuyoshi AOKI、Hiroyasu SATO、Sen-ichi NARITA
DOI:10.1248/cpb.37.1647
日期:——
Synthesis of homoisocarbacyclin has been achieved efficiently by a general strategy with stereo- and regiochemical control. One of homoisocarbacyclin derivatives, 3-oxa homoisocarbacyclin analog (4), was shown to be potently active in inhibiting gastric ulcer. Another analog, conjugated diene derivative (5), was found to have a biological profile similar to prostacyclin.
已经通过立体和区域化学控制的一般策略有效地实现了高异碳环素的合成。均异碳环素衍生物之一,3-氧杂均碳环素类似物(4)被证明在抑制胃溃疡方面具有有效活性。发现另一种类似物,共轭二烯衍生物(5),具有与前列环素相似的生物学特性。