The invention relates to substituted dihydropyrazolo pyrazine carboxamide derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and diabetes, and also urogenital and ophthalmic disorders.
Benzopiperidine derivatives represented by formula (I), salts thereof or hydrates thereof, processes for producing the same and drugs comprising the same:
wherein the variables are as described in the specification. These compounds are useful as drugs efficacious in the prevention and treatment of these various inflammatory diseases and immunologic diseases, such as rheumatoid arthritis, atopic dermatitis, psoriasis, asthma, and rejection reaction accompanying organ transplantation.
A phosphane‐catalyzed [3+3] annulation of azomethineimines with ynones has been developed. Under mild reaction conditions, the reaction proceeds smoothly to afford tricyclic dinitrogen‐fused heterocyclic compounds in moderate to excellent yields with moderate to excellent stereoselectivies. Using a chiral phosphine as the catalyst, the reaction could work to give the cycloadduct in moderate yield
method to access functionalized aliphatic acidesters using silylperoxyacetals as alkyl radical precursors with a terminal ester moiety is described. The reaction proceeds via the in situ generation and subsequent functionalization of alkyl radicals, affording synthetically valuable aliphatic acid derivatives. A novel strategy for the synthesis of hydroxy acid derivatives via a C−O bond formation process
描述了使用甲硅烷基过氧缩醛作为具有末端酯部分的烷基自由基前体获得官能化脂肪酸酯的催化方法。该反应通过烷基自由基的原位生成和随后的官能化进行,得到具有合成价值的脂肪酸衍生物。还开发了一种通过 CO 键形成过程合成羟基酸衍生物的新策略。
Catalytic Asymmetric [4 + 3] Annulation of <i>C</i>,<i>N</i>-Cyclic Azomethine Imines with Copper Allenylidenes
The first asymmetric decarboxylative [4 + 3] annulation of propargylic carbamates with C, N-cyclic azomethineimines has been developed successfully by a copper- N-heterocyclic carbine system. This strategy led to a series of optically active isoquinoline-fused triazepine derivatives in good yields and with excellent enantio- and diastereoselectivities. Remarkably, Cu-allenylidene intermediates play