5043-07-2Relevant academic research and scientific papers
PHARMACEUTICAL COMPOSITION AND THE USE THEREOF, AND APPLICATION REGIME OF SAID PHARMACEUTICAL COMPOSITION FOR ON-DEMAND CONTRACEPTION
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Page/Page column 134; 165, (2016/04/26)
The invention relates to a pharmaceutical composition for non-hormonal, on-demand contraception and to processes for preparing this pharmaceutical composition. The latter comprises 2H-indazole as novel EP2 receptor antagonists in combination with COX inhi
Ni-catalyzed carboxylation of C(sp2)- and C(sp3)-O bonds with CO2
Correa, Arkaitz,Leon, Thierry,Martin, Ruben
, p. 1062 - 1069 (2014/02/14)
In recent years a significant progress has been made for the carboxylation of aryl and benzyl halides with CO2, becoming convenient alternatives to the use of stoichiometric amounts of well-defined metal species. Still, however, most of these processes require the use of pyrophoric and air-sensitive reagents and the current methods are mostly restricted to organic halides. Therefore, the discovery of a mild, operationally simple alternate carboxylation that occurs with a wide substrate scope employing readily available coupling partners will be highly desirable. Herein, we report a new protocol that deals with the development of a synergistic activation of CO2 and a rather challenging activation of inert C(sp2)-O and C(sp3)-O bonds derived from simple and cheap alcohols, a previously unrecognized opportunity in this field. This unprecedented carboxylation event is characterized by its simplicity, mild reaction conditions, remarkable selectivity pattern and an excellent chemoselectivity profile using air-, moisture-insensitive and easy-to-handle nickel precatalysts. Our results render our method a powerful alternative, practicality and novelty aside, to commonly used organic halides as counterparts in carboxylation protocols. Furthermore, this study shows, for the first time, that traceless directing groups allow for the reductive coupling of substrates without extended π-systems, a typical requisite in many C-O bond-cleavage reactions. Taking into consideration the limited knowledge in catalytic carboxylative reductive events, and the prospective impact of providing a new tool for accessing valuable carboxylic acids, we believe this work opens up new vistas and allows new tactics in reductive coupling events.
Substituted-aryl 7-aza[2.2.1]bicycloheptanes for the treatment of disease
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, (2008/06/13)
The invention provides compounds of Formula I: wherein the stereochemistry of the of the 7-azabicyclo[2.2.1]heptane ring is 1S, 2R, 4R and the nitrogen substituent at the C-2 carbon has the exo orientation; W is -Q, —C═C-Q, or —C≡C-Q; and Q is as defined
Azabicyclic compounds for the treatment of disease
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Page 38, (2010/02/06)
The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1-2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1-2 substitutents independently selected from R3. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which α7 is known to be involved.
Reductive Methylation of Naphthoic Esters
Basu, Basudeb,Mukherjee, Debabrata
, p. 105 - 106 (2007/10/02)
Reductive methylation of the naphthoic esters (3), (9), (13), and (15) was carried out in distilled liquid ammonia in the presence of sodium to give the esters (19), (20), (21), and (22), respectively.
