Synthesis of novel and photolabile philanthotoxin analogs: Glutamate receptor antagonists
摘要:
The synthetic methods for 27 novel and photolabile philanthotoxin analogs are described. Most analogs were synthesized by two general methods with modifications of these methods where necessary.
nitroarenes. The important features are the introduction of N-acetoxyacetamide as a new directing group, redox-neutral annulation, an additive-free approach, wide functional group tolerance, an intramolecular version, and a one-pot reaction of nitroarenes. The method was further extended to the synthesis of potent higher analogues of indole, viz., pyrrolo[3,2-f]indoles and dibenzo[a,c]carbazoles. In addition
N-乙酰氧基乙酰苯胺的一般和有效的铑催化氧化还原中性环化,容易从硝基芳烃中获得,与炔烃已经完成,用于合成取代的吲哚衍生物。从各种取代的N-乙酰氧基乙酰苯胺和对称/不对称炔烃中获得了范围广泛的取代 2,3-二芳基吲哚,产率从良好到优异。所开发的方法成功地与N-乙酰氧基乙酰苯胺的合成相结合,用于从硝基芳烃中有效地一锅法合成吲哚。重要的特点是引入了N-乙酰氧基乙酰胺作为新的导向基团,氧化还原中性环化,无添加剂方法,广泛的官能团耐受性,分子内形式和硝基芳烃的一锅反应。该方法进一步扩展到合成有效的高级吲哚类似物,即。、吡咯并[3,2- f ]吲哚和二苯并[ a , c ]咔唑。此外,基于潜在芳基-Rh中间体的分离和化学计量研究,提出了一种合理的机制。
Highly Efficient Stereoselective Catalytic C(sp<sup>3</sup>)H Insertions with Donor Rhodium Carbenoids Generated from Cyclopropenes
Rings of five and six: Donor alkenyl rhodiumcarbenoidsgeneratedfrom 3,3‐dimethylcyclopropenylcarbinols exhibit high reactivity in intramolecular CHinsertions. The reactions proceed under remarkably mild conditions, tolerate the presence of the free hydroxy group, and afford an efficient and stereoselective access to a variety of functionalized carbocycles and oxygen heterocycles.
The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.
The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other conditions or disorders associated with kinases.
The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.