BIOLOGICALLY ACTIVE COMPOUNDS VIA CHIRAL AROMATICS

描述：在本更新申请中，主要研究者 他说，研究正在继续对新的合成路线， 医学上重要的化合物，凭借新的，立体化学 手性配体合成新途径 用于催化合成反应继续进行。 他指出，联芳基化合物 具有高程度的对映体纯度的预测基于不对称 Ullmann反应及其在全合成 （-）-棉酚正在进行中。 他还指出，手性胺作为 特定的试剂、中间体或催化剂， 对映选择性反应也在研究中。 首席研究员报告说，继续他非常成功的 使用各种亲核试剂对萘进行加成， 亲电试剂导致了吗啡烷衍生物的重要路线， 其他生物活性物质，他目前正在应用 这一新的方法，（-）-曲醌，抑制剂的IL-1释放。 这表明，各种各样的类似物的triptoquinone是 类风湿关节炎的研究，如果化学证明 成功 首席研究员指出，研究也在 完成aphidocolin合成的进展（通过萘 方法），并制备新的C2-对称系统（六氢喹啉）， 制造具有螺旋轴的多肽。 最后指出，研究达到一些海洋 复合阵列中的恶唑和噻唑形式的多肽， 这些高活性物质被发现 抗真菌、抗生素、HIV抑制剂、细胞毒性和抗 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.