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研發含□□丁烯酸內酯及四氫咪□苯二氮雜草酮類化合物作為抗癌與抗愛滋試劑;藉由有機矽β–穩定效應促進羅氏II型斷裂反應
Thesis

研發含□□丁烯酸內酯及四氫咪□苯二氮雜草酮類化合物作為抗癌與抗愛滋試劑;藉由有機矽β–穩定效應促進羅氏II型斷裂反應

梅乃文
Masters, National Tsing Hua University
2000

Abstract

□□丁烯酸內酯四氫咪□苯二氮雜草酮丁烯酸內酯 butenolidetetrahydroimidazobenzodiazepinoneNorrish type II
In this thesis, we designed novel butenolide derivatives of nucleobases as anticancer agents. We also prepared a tetrahydroimidazobenzodiazepinone analog as anti-HIV agent. Furthermore, silicon-promoted Norrish type II cleavage by a □-stabilization effect was investigated.In part 1 of this thesis, a series of butenolide-containing 6-chloropurine having an active double bond was synthesised to inhibit enzymes crucial to metabolic pathways in cell division. Those compounds exhibited moderate anticancer activity.In part 2 of this thesis, internal alkylation of N3-position of an adenine acyclonucleoside with its alkyl halide side chain occurred. The resultant tetrahydroimidazobenzodiazepinone analog exhibited antiviral activity in vitro.In part 3 of this thesis, photolysis of the □-silylated and non-silylated bicycloalkanones showed compounds bearing an SIMe3 at □ position molecule have a higher quantum yields and rate constants. The trimethylsilyl group, being synperiplanar to the □-hydrogen, provided greater driving force than the trimethylsilyl group being anticlinalin the cleavage of the C-H bond.

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