63074-07-7Relevant articles and documents
Why we might be misusing process mass intensity (PMI) and a methodology to apply it effectively as a discovery level metric
Monteith, Edward R.,Mampuys, Pieter,Summerton, Louise,Clark, James H.,Maes, Bert U. W.,McElroy, C. Robert
, p. 123 - 135 (2020)
Process mass intensity (PMI) is a key mass-based metric to evaluate the green credentials of an individual or sequence of reactions during process and chemical development. The increasing awareness to consider greenness as early as the initial discovery level, requires a set of parameters suitable to assess it at this stage of development, and guidelines to apply them correctly. This paper evaluates when and how PMI can be used in a correct manner. Different simulations for key reactions in the organic synthesis toolbox-i.e. amide bond formation and Mitsunobu reactions-illustrate that PMI can easily be misleading without due consideration of yield, concentration and molecular weight of reactants and product. A fair appraisal of the green potential of different methodologies therefore requires careful analysis of the examples and metrics data generated.
PREPARATION AND UTILITY OF SUBSTITUTED QUINAZOLINE COMPOUNDS WITH ALPHA-ADRENERGIC BLOCKING EFFECTS
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Page/Page column 71, (2008/06/13)
The present disclosure is directed to modulators of alpha-adrenergic receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or management of hypertension, cardiac failure, prostatitis, and benign prostatic hyperplasia, and any other condition in which it is beneficial to modulate an alpha-adrenergic receptor.
Preparation of amides and quinazoline derivatives
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, (2008/06/13)
The present invention relates to a process for the preparation of amides, comprising reacting amines with carboxylic acids in the presence of silicon amines. The present invention further relates to a process for the preparation of quinazoline derivatives, comprising reacting amines with carboxylic acids in the presence of silicon amines to obtain amides and contacting the resultant amides with quinazoline.