BIOLOGICALLY ACTIVE COMPOUNDS VIA CHIRAL AROMATICS

描述：在这份续签申请中，首席调查员 国家正在继续研究新的合成路线，以 药用上重要的化合物，凭借新的立体化学 特定反应和合成手性配体的新的有效途径 对于催化合成反应仍在继续。他指出，联芳基 基于不对称理论预测对映体的高度不对称 乌尔曼反应及其在全合成中应用 (-)-棉酚正在进行中。他还指出，手性胺作为 一系列特定的试剂、中间体或催化剂 对映体选择性反应也在研究中。 首席调查员报告说，继续他非常成功的 使用多种亲核试剂与萘加成 亲电性导致了重要的吗啡烷衍生物和 其他生物活性物质，他目前正在申请 这一新的方法学用于IL-1释放的抑制剂(-)-曲普醌。 建议将三苯并三酚的各种类似物 如果化学成分证明，可用于类风湿性关节炎研究 成功。首席研究员指出，这项研究也在 以萘为原料完成Aphidoclin合成的研究进展 方法)，并制备新型C2对称体系(六氢黄烷)以 制造具有螺旋(螺旋)轴的多肽。 最后有人说，研究人员将到达一些海洋 在复杂阵列中以恶唑和噻唑形式存在的多肽 这些高活性物质已被发现 抗真菌、抗生素、艾滋病毒抑制剂、细胞毒性和抗真菌药物 关节炎。

DESCRIPTION: In this renewal application, the principal investigator states that studies are continuing on novel synthetic routes to medicinally important compounds, by virtue of new, stereochemically specific reactions and that novel and efficient routes to chiral ligands for catalytic synthetic reactions continue. He indicates that biaryls with high degrees of enantiopurity are forecast based on asymmetric Ullmann reactions and that application of this to a total synthesis of (-)-Gossypol is in progress. He also notes that chiral amines as specific reagents, intermediates, or catalysts for a host of enantioselective reactions are also being studied. The principal investigator reports that continuing his very successful additions to naphthalenes using a variety of nucleophiles and electrophiles has led to important routes to morphinane derivatives and other biologically active substances and that he is currently applying this new methodology to (-)-Triptoquinone, an inhibitor of IL-1 release. It is suggested that a variety of analogs of triptoquinone are to be accessible for rheumatoid arthritis study if the chemistry proves successful. The principal investigator notes that studies also are in progress to complete the synthesis of aphidocolin (via the naphthalene method) and prepare novel C2-symmetric systems (hexahydrochrysene) to make polypeptides with a helical (screw) axis. It is finally stated that studies to reach a number of marine polypeptides in the form of oxazoles and thiazoles in complex arrays are in progress and that these highly active substances have been found to be anti-fungal, antibiotic, HIV-inhibitors, cytotoxic, and anti- arthritic.