- PROCESS FOR THE SYNTHESIS OF DEUTERATED CAPSAICIN, CAPSAICINOIDS AND SYNTHETIC CAPSAICIN ANALOGS
-
The present application provides novel processes for the synthesis of deuterated intermediates of capsaicinoids, particularly II, III, IV and V of capsaicinoids, relating to pharmaceutical applications. The invention also provides novel intermediates of compounds of formula IX, XIV, XV, XVI, XVII, XVIII, XX and XXI utilized in the process of making deuterated capsaicin II, III, IV and V.
- -
-
Page/Page column 27
(2021/01/29)
-
- Targeting RAS-RAF pathway significantly improves antitumor activity of Rigosertib-derived platinum(IV) complexes and overcomes cisplatin resistance
-
RAS-RAF pathway presents a valuable target for the cancer treatment due to its important roles in the regulation of tumor proliferation, apoptosis and the obtained resistance. To explore such target a RAS/CRAF interference agent, was therefore conjugated
- Liu, Zhikun,Wang, Meng,Wang, Hengshan,Fang, Lei,Gou, Shaohua
-
-
- Aminocarbonylation of Aryl Tosylates to Carboxamides
-
The palladium - catalyzed aminocarbonylation of aryl tosylates with amines is reported. Suitable conditions were identified by high throughput reaction screening and then further optimized. The substrate scope of the reaction with respect to the aryl tosylate component and the amine component are reported. Competitive aminolysis of the aryl tosylates to afford the amine toluenesulfonamides and the phenol was not observed.
- Chung, Seungwon,Sach, Neal,Choi, Chulho,Yang, Xiaojing,Drozda, Susan E.,Singer, Robert A.,Wright, Stephen W.
-
supporting information
p. 2848 - 2851
(2015/06/16)
-
- PROCESSES FOR PREPARING (E)-STYRYLBENZYLSULFONE COMPOUNDS AND USES THEREOF FOR TREATING PROLIFERATIVE DISORDERS
-
Processes for preparing (E)-2,4,6-(Trimethoxystyryl)-3-O-Phosphate Disodium-4-Methoxybenzyl Sulfones and uses thereof as antiproliferative agents, including, for example, anticancer agents, and as radioprotective and chemoprotective agents.
- -
-
Page/Page column 29
(2010/06/22)
-
- PHARMACEUTICAL COMPOUNDS
-
This application describes substituted 1,3,4,6,7,11b-hexahydro-benzo(a)quinolizine compounds, pharmaceutical compositions containing them, processes for making them and their therapeutic methods.
- -
-
Page/Page column 32
(2010/04/30)
-
- Design, synthesis, and biological evaluation of (E)-styrylbenzylsulfones as novel anticancer agents
-
Cell cycle progression is regulated by cyclins and cyclin-dependent kinases, which are formed at specific stages of the cell cycle and regulate the G1/S and G2/M phase transitions, employing a series of "checkpoints" governed by phosphorylation of their substrates. Tumor development is associated with the loss of these checkpoint controls, and this provides an approach for the development of therapeutic agents that can specifically target tumor cells. Here, we describe the synthesis and SAR of a novel group of cytotoxic molecules that selectively induce growth arrest of normal cells in the G1 phase while inducing a mitotic arrest of tumor cells resulting in selective killing of tumor cell populations with little or no effect on normal cell viability. The broad spectrum of antitumor activity in vitro and xenograft models, lack of in vivo toxicity, and drug resistance suggest potential for use of these agents in cancer therapy.
- Reddy, M. V. Ramana,Mallireddigari, Muralidhar R.,Cosenza, Stephen C.,Pallela, Venkat R.,Iqbal, Nabisa M.,Robell, Kimberly A.,Kang, Anthony D.,Reddy, E. Premkumar
-
-
- Palladium-catalyzed carbonylation of aryl tosylates and mesylates
-
A general protocol for the palladium-catalyzed carbonylation of aryl tosylates and mesylates to form esters has been developed using a catalyst system derived from Pd(OAc)2 and the bulky, bidentate dcpp ligand. The system operates under mild conditions: atmospheric CO pressure and temperatures of 80-110 °C. A broad substrate scope has been demonstrated allowing carbonylation of electron-rich, electron-poor, and heterocyclic tosylates and mesylates, and the reaction shows wide functional group tolerance. Copyright
- Munday, Rachel H.,Martinelli, Joseph R.,Buchwald, Stephen L.
-
p. 2754 - 2755
(2008/09/19)
-
- Suzuki-Miyaura coupling of aryl tosylates catalyzed by an array of indolyl phosphine-palladium catalysts
-
A family of indolyl phosphine ligands was applied to Suzuki-Miyaura cross-coupling of aryl tosylates. Catalyst loading can be reduced to 0.2 mol % for coupling of nonactivated aryl tosylate. A challenging example for room temperature coupling is realized. The scope of this highly active Pd/L2 system can be extended to other boron nucleophiles, including trifluoroborate salts and boronate esters. The ligand structural comparisons toward the reactivity in tosylate couplings are also described.
- So, Chau Ming,Lau, Chak Po,Chan, Albert S. C.,Kwong, Fuk Yee
-
p. 7731 - 7734
(2008/12/22)
-
- Covalently linked acceptor - Donor systems based on isoquinoline N-oxide acceptor: Photoinduced electron transfer produces dual-channel luminescent systems that evolve chemically to photohydroxylation of the aromatic donor
-
Acceptor-donor compounds containing the isoquinoline N-oxide acceptor and (methoxy)nbenzene (n = 0, 1, 2, 3) electron donors were studied. The two chromophores are connected by a CH2 bridging unit. All acceptor-donor compounds exhibi
- Collado, Daniel,Perez-Inestrosa, Ezequiel,Suau, Rafael
-
p. 3574 - 3584
(2007/10/03)
-