首页> 外国专利> The process of su00ecntese anti tumour compounds: (-) - hyrtiosal, (+) - hyrtiosal, (-) - 16 - epi - hyrtiosal and (+) - 16 - epi - hyrtiosal

The process of su00ecntese anti tumour compounds: (-) - hyrtiosal, (+) - hyrtiosal, (-) - 16 - epi - hyrtiosal and (+) - 16 - epi - hyrtiosal

机译:西尼特抗肿瘤化合物的过程:(-)-宫缩,(+)-宫缩,(-)-16-发作-宫缩和(+)-16-epi-宫

摘要

"The process of su00ecntese anti tumour compounds: (-) - hyrtiosal, (+) - hyrtiosal, (-) - 16 - epi - hyrtiosal and (+) - 16 - epi - hyrtiosal".Refers to the preparation of a natural product of marine origin and their stereoisomers from the copu00e1lico acid.Isolated from the commercial copaiba oil containing the two forms enantiomu00e9ricas, i.e., the acid (+) and (-) - copu00e1lico copu00e1lico.The (-) - hyrtiosal is the natural product isolated from the methanol extract of marine sponge hyrtios erectus by Iguchi and colab. [J. org.Chem 57: 522 - 524 (1992)], and has antiproliferative activity against the cells of the type KB (CI ~ 50 ~ 3 - 10 109 G / ml).In this case we 're communicating the synthesis of (-) - hyrtiosal its enantiomer of (+) - hyrtiosal, and its epu00edmeros in C - 16, (-) - 16 - epi - hyrtiosal and (+) - 16 - epi - hyrtiosal,From the acid ( sym ) - copu00e1lico in 11 steps.The total income for each isomer were: 4.8% to (-) - hyrtiosal (1), 4.2% for (+) - hyrtiosal (2), 6.8% to (-) - 16 - epi - hyrtiosal (22) and 6.0% for (+) - 16 - epi - hyrtiosal (23).
机译:“抗肿瘤化合物的过程:(-)-眼泪,(+)-眼泪,(-)-16-Epi-眼泪和(+)-16-epi-眼泪”。参考准备来源于copcopulicic acid的海洋天然产物及其立体异构体。从商购的copaiba油中分离得到,包含两种形式的对映体,即酸(+)和(-)-copicolicic。 (-)-百草枯是由Iguchi和colab从海洋海绵状直立的甲醇提取物中分离得到的天然产物。 [J. org.Chem 57:522-524(1992)],并且对KB型细胞(CI〜50〜3-10 <109> G / ml)具有抗增殖活性。在这种情况下,我们正在传达合成(-)-垂体的对映体(+)-垂体的对映体,及其在C-16(-)-16-epi-垂体和(+)-16-epi-垂体的对映体,由酸(< sym>)-cop u00e1lico分11个步骤。每种异构体的总收入为:(-)-垂体(1)的4​​.8%,(+)-垂体(2)的4.2%,(-)的6.8%- 16-Epi-眼泪(22)和6.0%(+)-16-Epi-眼泪(23)。

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