五味子甲素及其类似物的全合成

TOTAL SYNTHESIS OF (±) DEOXYSCHISANDRIN AND ITS ANALOGUES

目的:合成五味子甲素及其类似物。方法:采用DDQ(2 ,3二氯5 ,6二氰基1 ,4苯醌) 做为氧化偶合试剂进行分子内非酚氧化偶合,并用1HNMR,MS和EA等进行化合物结构鉴定。结果:合成了21 个化合物,其中10 个为新化合物(5 ,6 ,8,9 ,11 ,12 ,14 ,15 ,17 和20) 。结论:初步药理筛选表明,化合物10 ～15 对环氧酶活性抑制作用都较强,提示这些化合物可能有抗炎活性;化合物19 ～21

AIM: To synthesize (±) deoxyschisandrin and its analogues. METHODS: The compounds are readily prepared by intramolecular oxidative coupling with 2,3 dichloro 5,6 dicyano 1,4 benzoquinone (DDQ) in trifluoroacetic acid (TFA). The structures of these compounds are confirmed by MS, 1HNMR and EA. RESULTS: Twenty one compounds have been synthesized among them 10 (5, 6, 8, 9, 11, 12, 14, 15, 17 and 20) are new compounds. CONCLUSION: The results of preliminary pharmacological tests on compounds have showen that compounds 10～15 have anti inflammation activities and compounds 19～21 have anti convulsive activities.