3-~3H-4β,15-二乙酰氧基-8α-(3-甲基丁酰氧基)-3α-羟基-12,13-环氧单端孢霉-9-烯的合成

SYNTHESIS OF 3-~3H -4β,15-DIACETOXY 8a-(3- METHYLBUTYRYLOXY)-3a-HYDROXY-12, 13-EPO-XYTRICHOTHEC-9-ENE

摘要: <正> 4β,15-二乙酰氧基-8α-(3-甲基丁酰氧基)-3α-羟基-12,13-环氧单端孢霉-9-烯(简称T-2毒素,分子式见反应式中I)属于一种真菌毒素,人畜中毒后可引起呕吐、大量出血、皮肤奇痒、痉挛、抽搐等各种症状,严重者可致死亡。为了建立放射免疫测定法和进行皮肤毒理学的研究,制备了~3H-T-2毒素。

Abstract: 3-3H-4β, 15-diacetoxy, 8α- (3-methylburyloxy) -3α-hydroxy-12, 13-epoxy trichothec-9-ene is synthetized by oxidizing the C-3-hydroxy to ketone . It is reduced with NaB3H4 to a mixture of epimers which are separable by high thin-layer chromatography. The specific activity is 629 GBq/mmol and radio-themical parity is over 98%. Specific activity of this tritium labeled T-2-toxin is higher than that by Wallace.