与异恶唑合成。第二部分 异恶唑并[2,3- a ]-吡啶盐重排为5,6-二氢-4 H-呋喃[3,2 - b ]吡啶-2-酮
摘要:
用沸腾的乙酸酐对四氢-4-氧代恶唑啉[2,3- a ]吡啶鎓盐(1)和(12)进行简短处理,得到5,6-二氢-4 H-呋喃[3,2-b]吡啶- 2个(4)和(13)。化合物(4)的结构已通过完全氢化成哌啶-2-基乙酸并通过X射线衍射证明。2-甲基异恶唑啉代-[2,3-a]吡啶鎓盐(11)没有进行重排;这表明是通过除去2位上的氢原子形成的酮基中间体。5-溴衍生物(22)没有产生呋喃吡啶。发生吡啶或异恶唑环的断裂。
these transporters should not be addressed by such an inhibitor. A high-throughput screen against a library of ∼3 million compounds was performed to find a small molecule with this challenging potency and selectivity profile. The N-(1H-pyrazol-4-yl)quinoline-4-carboxamides were identified as an excellent starting point for further compound optimization. After extensive structure-activity relationship explorations
[EN] MACROCYCLIC DERIVATIVES FOR THE TREATMENT OF PROLIFERATIVE DISEASES<br/>[FR] DÉRIVÉS MACROCYCLIQUES POUR LE TRAITEMENT DE MALADIES PROLIFÉRATIVES
申请人:PFIZER
公开号:WO2013132376A1
公开(公告)日:2013-09-12
The invention relates to compounds of formula (Φ) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.
1-Substituted Cyclopentylamines from Nitriles and Tetramethylenebismagnesium Dibromide in the Presence of Ti(O<i>i</i>Pr)<sub>4</sub>
作者:Olesya A. Tomashenko、Andrei E. Rudenko、Viktor V. Sokolov、Alexander A. Tomashevskiy、Armin de Meijere
DOI:10.1002/ejoc.200900817
日期:2010.3
Various 1-substitutedcyclopentylamines (25 examples, 10― 89 % yield) have been prepared according to a one-pot procedure by the addition of tetramethylenebismagnesiumdibromide in the presence of Ti(OiPr) 4 to aliphatic, aromatic and heteroaromatic nitriles, respectively.
Inhibitors Of Hepatitis C Virus Protease, And Compositions And Treatments Using The Same
申请人:Collins Raymond Michael
公开号:US20070249637A1
公开(公告)日:2007-10-25
The present invention provides compounds of formula (I), (II) or (IV), or pharmaceutically acceptable salts and solvates thereof, which are useful as inhibitors of the Hepatitis C virus (HCV) protease enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals, including humans. The present invention also provides pharmaceutical compositions comprising compounds of formula (I), (II) or (IV), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formulas (I), (II) and (IV).
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.