1,720,968 research outputs found

    Process for the preparation of brinzolamide

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    The present invention relates to a process for the preparation of Brinzolamide, or 2H-thieno[3,2-e]-1, 2-thiazin-6-sulfonamide, 4-(ethyl amino)-3, 4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide,(4R)- via intermediates 2,3-dihydro-4H-thieno[3,2-e]-1, 2-thiazin-4-ones, 1,1-dioxide. Further objects of the present invention are the intermediates mentioned above and other intermediates of the synthesis

    Process for the preparation of testosterone

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    The present invention relates to an industrial process for the reduction of 4-androstene-3,17-dione in order to obtain testosterone using a particularly stable and selective enzyme produced in a recombinant manner

    BIOCATALYZED SYNTHESIS OF TESTOSTERONE

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    We have recently developed and submitted for a patent a new industrial process for the production of testosterone making use of biocatalysis. In particular, a non commercial enzyme was proposed to overcome a critical steps in the organic synthesis of the hormone: the regio- and stereo-specific conversion of 4-androstene-3,17-dione to testosterone. Design of the process was based on a strategy starting with the identification of the enzyme by crossed bioinformatics and literature screening: the chosen candidate was the 17P-hydrosteroid dehydrogenase type 5 from mouse. The coding sequence for the enzyme was cloned in a vector suitable for its expression, in fusion with an His-tag, in E.coli. Small scale preparations of the recombinant enzyme were initially set up and activity tests on the desired substrate were performed, using the co-factor NADPH or NADH. The small scale purifications allowed verification of the product obtained in terms of regio- and stereo-selectivity and yield, evaluation of thermal stability of the enzyme, kinetic analysis of the reaction and choice of an adequate partial organic mixture to work with. A protocol for purification of the enzyme from medium scale cultures was then drawn and performed. The amount of enzyme obtained from these preparations, in combination with the commercially available D-glucose dehydrogenase required for the recycling of the cofactor NADH, allowed the conversion of milligrams of androstendione. Conditions for higher scale synthesis of testosterone are going to be developed

    Going Beyond Counting First Authors in Author Co-citation Analysis

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    The present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed

    Variations on the Author

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    “Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship

    Appropriate Similarity Measures for Author Cocitation Analysis

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    We provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis

    Structure and reactivity of molecular ions of isomeric pyrroloquinolinones and benzoquinolizinones.

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    The structure and mass spectrometric behaviour of molecular species of two benzo[ij]quinolizin-5-ones and one pyrrol[3,2,1-ij]quinolin-4-one were studied in detail with the aid of mass-analysed ion kinetic energy spectrometry and ion trapping experiments. Whereas in the usual electron impact spectra obtained with a double-focusing instrument clear differences are present among the three isomeric componds, the unimolecular fragmentation processes of the related M+. indicate the occurrence of isomerization processes to give a common structure. Significantly, under ion trap conditions nearly identical electron impact spectra are obtained; such unexpected behaviour was explained by either the presence of the buffer gas or the occurrence of different ionizing phenomena, leading to lower energy deposition in the molecular species. Under fast atom bombardment conditions, an acid-catalysed isomerization process occurs

    REGIOSPECIFIC SYNTHESIS OF 1H,5H-BENZO[IJ]QUINOLIZIN-5-ONE AND 3H,5H-BENZO[IJ]QUINOLIZIN-5-ONE DERIVATIVES

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    Regiospecific separate syntheses of the new 1H,5H- and 3H,5H-benzo[ij]quinolizin-5-one derivatives exploiting 2-bromo-10-hydroxy-7-methyl-1H,2H,3H,5H-benzo[ij]quinolizin-5-one as common key intermediate are described. The structure or 2-bromo-10-hydroxy-7-methyl-1H,2H,3H,5H-benzo[ij]quinolizin-5-one (*) has been determined by X-ray analysis. Crystal data: a = 7.248(3), b = 18.40(1), c = 9.132(7) angstrom, beta = 106.08(5)-degrees; space group P2(1)/c; Z = 4
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