- Recycled Pd/C-Catalyzed Heck Reaction of 2-Iodoanilines under Ligand-Free Conditions
-
Recyclable Pd/C-catalyzed Heck reaction of 2-iodoanilines with acrylate has been developed. The reaction occurred readily in 1,4-dioxane using Pd/C (10 wt%) as catalyst under ligand-free conditions, and the cross-coupling products were obtained with medium to high yield. Gram-scale reactions and recycling of the catalyst were also demonstrated.
- Zhou, Xiao-Yu,Chen, Xia,Wang, Liang-Guang
-
supporting information
p. 5364 - 5370
(2017/12/14)
-
- Palladium catalyzed Heck reaction of 2-iodoanilines under ligand-free conditions in air
-
Palladium catalyzed Heck reaction of 2-iodoanilines and acrylate has been developed. The palladium catalyzed Heck reaction of 2-iodoanilines can readily occur in CH3CN using Pd(OAc)2 (5.0 mol%) as catalyst, NEt3 as base un
- Chen, Xia,Zhou, Xiao-Yu,Wang, Liang-Guang
-
supporting information
p. 2096 - 2102
(2017/10/26)
-
- ALPHA-CINNAMIDE COMPOUNDS AND COMPOSITIONS AS HDAC8 INHIBITORS
-
The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
- -
-
Paragraph 0886; 0887
(2016/10/04)
-
- Continuous Consecutive Reactions with Inter-Reaction Solvent Exchange by Membrane Separation
-
Pharmaceutical production typically involves multiple reaction steps with separations between successive reactions. Two processes which complicate the transition from batch to continuous operation in multistep synthesis are solvent exchange (especially high-boiling- to low-boiling-point solvent), and catalyst separation. Demonstrated here is membrane separation as an enabling platform for undertaking these processes during continuous operation. Two consecutive reactions are performed in different solvents, with catalyst separation and inter-reaction solvent exchange achieved by continuous flow membrane units. A Heck coupling reaction is performed in N,N-dimethylformamide (DMF) in a continuous membrane reactor which retains the catalyst. The Heck reaction product undergoes solvent exchange in a counter-current membrane system where DMF is continuously replaced by ethanol. After exchange the product dissolved in ethanol passes through a column packed with an iron catalyst, and undergoes reduction (>99 % yield).
- Peeva, Ludmila,Da Silva Burgal, Joao,Heckenast, Zsofia,Brazy, Florine,Cazenave, Florian,Livingston, Andrew
-
p. 13576 - 13579
(2016/10/21)
-
- 2,3-substituted indole compounds as anti-inflammatory and analgesic agents
-
This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the following: (a) an optionally substituted phenyl, (b) an optionally substituted 6-membered monocyclic aromatic group containing one, two, three or four nitrogen atom(s), (c) an optionally substituted 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, (d) an optionally substituted C3-7 cycloalkyl and (e) an optionally substituted benzo-fuzed heterocycle; R1 is hydrogen, C1-4 alkyl or halo; R2 and R3 are independently hydrogen, OH, C1-4 alkoxy, C1-4 alkyl or C1-4 alkyl substituted with halo, OH, C1-4 alkoxy or CN; X is independently selected from H, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 alkyl)amino and CN; and n is 0, 1, 2, 3 and 4.This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.
- -
-
-
- Efficient synthesis of [6-chloro-2-(4-chlorobenzoyl)-1H-indol-3-yl]acetic acid, a novel COX-2 inhibitor
-
The synthesis of 6-chloro-2-(4-chlorobenzoyl)-1H-indol-3-ylacetic acid (1), a selective cyclooxygenase 2 (COX-2) inhibitor, is described. The synthesis relied on a novel indole formation that involved an alkylation/1,4-addition/elimination/isomerization cascade. It was demonstrated that the entire sequence from sulfonamide 13 and bromoketone 14 to the desired indole (1) could be executed in a single pot.
- Caron, Ste?phane,Vazquez, Enrique,Stevens, Rodney W.,Nakao, Kazunari,Koike, Hiroki,Murata, Yoshinori
-
p. 4104 - 4107
(2007/10/03)
-