研究了四丁基癸酸铵(TBADT)光催化烷基吡啶的CH官能团。与烷基苯对应物不同,α-CH键的烷基化反应不会在2-和4-烷基吡啶的反应中进行,而对于3-烷基吡啶则勉强地进行,这允许在非苄基位置进行位点选择性的C(sp 3)-H官能化。观察到的非苄基位点选择性通过吡啶基在S H 2过渡态中的极性感应作用而合理化。在选定的案例中成功地连续进行了γ-官能化和α-溴官能化。
Order Flow, Transaction Clock, and Normality of Asset Returns
摘要:
The goal of this paper is to show that normality of asset returns can be recovered through a stochastic time change. Clark (1973) addressed this issue by representing the price process as a subordinated process with volume as the lognormally distributed subordinator. We extend Clark's results and find the following: (i) stochastic time changes are mathematically much less constraining than subordinators; (ii) the cumulative number of trades is a better stochastic clock than the volume for generating virtually perfect normality in returns; (iii) this clock can be modeled nonparametrically, allowing both the time‐change and price processes to take the form of jump diffusions.
DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF AS HIF ACTIVATORS
申请人:ALTENBURGER Jean-Michel
公开号:US20110294788A1
公开(公告)日:2011-12-01
The present invention relates to novel substituted dihydropyrazolone derivatives, to their preparation and to their therapeutic use as activators of the transcription factor HIF.
本发明涉及新型取代二氢吡唑酮衍生物,其制备以及作为转录因子HIF激活剂的治疗用途。
Site‐Specific Alkene Hydromethylation via Protonolysis of Titanacyclobutanes
作者:James A. Law、Noah M. Bartfield、James H. Frederich
DOI:10.1002/anie.202103278
日期:2021.6.21
Methyl groups are ubiquitous in biologically active molecules. Thus, new tactics to introduce this alkyl fragment into polyfunctional structures are of significant interest. With this goal in mind, a direct method for the Markovnikov hydromethylation of alkenes is reported. This method exploits the degenerate metathesis reaction between the titanium methylidene unveiled from Cp2Ti(μ-Cl)(μ-CH2)AlMe2
3-Carbonylamino-8-aminoisoquinoline compounds of formula (I):
variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the 3-carbonylamino-8-aminoisoquinoline compounds.
Synthesis, SAR, Crystal Structure, and Biological Evaluation of Benzoquinoliziniums as Activators of Wild-Type and Mutant Cystic Fibrosis Transmembrane Conductance Regulator Channels
fibrosis transmembrane conductance regulator (CFTR) is a cAMP-regulated epithelial chloride channel for which mutations cause cystic fibrosis. Here we have synthesized benzo[c]quinolizinium and benzo[f]indolo[2,3-a]quinoliziniumsalts (MPB) and performed a SAR to identify the structural basis for activation of the CFTR chloride channel. Synthesized compounds were evaluated on wild-type CFTR and on CFTR
[EN] INDAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME<br/>[FR] COMPOSÉS INDAZOLE UTILISÉS COMME INHIBITEURS DE KINASE ET MÉTHODE DE TRAITEMENT DU CANCER AVEC LESDITS COMPOSÉS
申请人:UNIV HEALTH NETWORK
公开号:WO2013053051A1
公开(公告)日:2013-04-18
The present teaching provide indazole compounds represented by Structural Formulae (I) or (I') or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as TTK protein kinase, polo-like kinase 4 (PLK4) and Aurora kinases having anticancer activity against breast cancer cells, colon cancer cells, and ovarian cancer cells.