Relevant articles and documents
All total 18 Articles be found
All total 18 Articles be foundScale-up of organic reactions in a pharmaceutical kilo-lab using a commercial microwave reactor
Lehmann, Hansjoerg,Lavecchia, Luigi
experimental part, p. 650 - 656 (2011/08/05)
A range of pharmaceutically relevant reactions were investigated for scale-up in a kilo-lab environment using a commercial batch microwave reactor. Typical scale-up issues are discussed, taking into account the specific limitations of microwave heating in large-scale experiments. Examples of scale-up from 15 mL to 1 L are presented and demonstrate that the synthesis of compounds on greater than 100 g scale is feasible in one batch. Aided by this new technology reaction times have been significantly reduced and the productivity of our scale-up laboratory has been enhanced. Production rates of several hundred grams per day were achieved using microwave technology. The article concludes with a brief discussion of advantages and disadvantages of this type of batch microwave reactor.
Scale-up of microwave-assisted reactions in a multimode bench-top reactor
Dallinger, Doris,Lehmann, Hansjoerg,Moseley, Jonathan D.,Stadler, Alexander,Kappe, C. Oliver
experimental part, p. 841 - 854 (2012/06/18)
An evaluation of a new bench-top microwave batch reactor that uses a single 1 L reaction vessel is presented. Several microwave-assisted organic reactions have been scaled-up, including Newman Kwart and Diels-Alder reactions, Pd-catalyzed cross-couplings, heterocycle synthesis, aromatic substitution, and a Knoevenagel condensation. A range of different solvents (high and low microwave absorbing), varying reaction times (4 s up to 2 h), and temperatures (120-250 °C) have been explored in these investigations. For all studied transformations, it was possible to perform a direct scale-up (up to 720 mL reaction volume) without changing the previously optimized reaction conditions achieved in a laboratory-scale single-mode microwave instrument (2-20 mL processing volume), obtaining similar isolated product yields. A scalability up to 360-fold, when moving from 3 mmol up to 1.08 mol, was demonstrated, and isolated product yields up to 300 g (2.5 mol scale) in a single run could be accomplished, providing the potential for a kilogram output per day for specific transformations by performing multiple sequential runs.
INHIBITORS OF PI3K-DELTA AND METHODS OF THEIR USE AND MANUFACTURE
-
Page/Page column 124-125, (2012/04/04)
The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
CONDENSED PYRIDINES AND PYRIMIDINES WITH TIE2 (TEK) ACTIVITY
-
Page 134, (2010/11/30)
-
COMPOSITIONS AND METHODS USING THE SAME FOR TREATMENT OF NEURODEGENERATIVE AND MITOCHONDRIAL DISEASE
-
Page/Page column 138; 139, (2015/09/22)
The present disclosure is directed, in part, to compounds, or pharmaceutically acceptable salts thereof, for the treatment and/or prevention of neurodegenerative disease and/or mitchonodrial disease including Parkinson's disease and Leigh's disease.
