Mechanistic aspects of aminium salt-catalyzed Diels-Alder reactions: The substrate ionization step
摘要:
Substituent effects in the aminium salt catalyzed Diels-Alder reactions of 2,3-dimethyl-1,3-butadiene with a series of meta and para substituted beta-methylstyrenes are used to probe detailed mechanistic aspects of these reactions. Kinetic studies were carried out using two different aminium salt catalysts and also electrochemically, using anodic potentials corresponding to the oxidation potentials of the aminium salts. Substituent effects in the equilibrium oxidations of the styrene substrates to the corresponding cation radicals were also studied, via oxidation potential measurements. The results indicate rate determining one electron oxidation of the sytrenes to their cation radicals via an outer sphere electron transfer.
[EN] ISOXAZOLINES AS INHIBITORS OF FATTY ACID AMIDE HYDROLASE<br/>[FR] ISOXAZOLINES EN TANT QU'INHIBITEURS DE L'HYDROLASE DES AMIDES D'ACIDES GRAS
申请人:INFINITY PHARMACEUTICALS INC
公开号:WO2010135360A1
公开(公告)日:2010-11-25
The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
Anti-Markovnikov Hydroazidation of Activated Olefins via Organic Photoredox Catalysis
作者:Nicholas P. R. Onuska、Megan E. Schutzbach-Horton、José L. Rosario Collazo、David. A. Nicewicz
DOI:10.1055/s-0039-1690691
日期:2020.1
bioactive and medicinally relevant molecules. Historically, the formal hydroazidation of simple activatedolefins and styrenes has proven difficult due to the inherent propensity of these compounds to oligomerize. Herein is disclosed a method for the anti-Markovnikov hydroazidation of activatedolefins, catalyzed by an organic acridinium salt under irradiation from blue LEDs. This method is applicable
THIOXOTHIAZOLIDINE DERIVATIVE HAVING RAS FUNCTION INHIBITORY EFFECT
申请人:Kataoka Tohru
公开号:US20140194412A1
公开(公告)日:2014-07-10
The present invention provides an anticancer drug having a Ras function inhibitory action.
The present invention provides a Ras function inhibitor comprising a compound represented by the formula (I′):
wherein each symbol is as defined in the present specification, or a salt thereof.
ISOXAZOLINES AS INHIBITORS OF FATTY ACID AMIDE HYDROLASE
申请人:Behnke Mark L.
公开号:US20110028478A1
公开(公告)日:2011-02-03
The present invention provides isoxazoline FAAH inhibitors of the formula (I):
or pharmaceutically acceptable forms thereof, wherein each of G, R
a
, R
b
, R
c
, and R
d
are as defined herein.
The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient.
The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
B(C
<sub>6</sub>
F
<sub>5</sub>
)
<sub>3</sub>
‐Catalyzed
<i>E</i>
‐Selective Isomerization of Alkenes
作者:Betty A. Kustiana、Salma A. Elsherbeni、Thomas G. Linford‐Wood、Rebecca L. Melen、Matthew N. Grayson、Louis C. Morrill
DOI:10.1002/chem.202202454
日期:2022.11.11
report the B(C6F5)3-catalyzed E-selective isomerization of alkenes. The transition-metal-free method is applicable across a diverse array of readily accessible substrates, accessing a broad range of synthetically useful products containing versatile stereodefined internal alkenes. Synthetic and computational mechanistic studies indicate that the isomerization proceeds along competing 1,2-hydride shift
Move along !:在此,我们报道了 B(C 6 F 5 ) 3 -催化的E -烯烃选择性异构化。不含过渡金属的方法适用于各种易于获得的底物,可获得范围广泛的合成有用产品,其中包含多功能立体定义的内部烯烃。合成和计算机理研究表明,异构化沿着竞争性 1,2-氢化物转移和氢化物提取途径进行。