The synthesis of amides remains one of the most important transformations and it is one of the more frequently performed reactions. In the pharmaceutical industry, the formation of the amide group is ...pivotal and among the more important transformations in the design of the synthetic plan. This review presents an overview of only very recent contributions, published in the last three years, to highlight the latest progress in this “dateless” reaction, with a special focus on metal‐free methodologies. New, more efficient and/or greener stoichiometric methods, as well as catalytic strategies, have been discussed, either for the “classic” coupling approach between an amine and a carboxylic acid (or its activated equivalent) or for more innovative approaches, mainly involving oxidation procedures to generate amides starting from amines.
The amide function is unarguably of primary importance, being the constituent of natural and synthetic polymers and found in a wide variety of bioactive molecules. This review will discuss specifically the very recent advances in the area of amide synthesis, specially focusing on metal‐free strategies, based either on stoichiometric or on catalytic methods that were published in the last three years.
Recently, application of the flow technologies for the preparation of fine chemicals, such as natural products or Active Pharmaceutical Ingredients (APIs), has become very popular, especially in ...academia. Although pharma industry still relies on multipurpose batch or semibatch reactors, it is evident that interest is arising toward continuous flow manufacturing of organic molecules, including highly functionalized and chiral compounds. Continuous flow synthetic methodologies can also be easily combined to other enabling technologies, such as microwave irradiation, supported reagents or catalysts, photochemistry, inductive heating, electrochemistry, new solvent systems, 3D printing, or microreactor technology. This combination could allow the development of fully automated process with an increased efficiency and, in many cases, improved sustainability. It has been also demonstrated that a safer manufacturing of organic intermediates and APIs could be obtained under continuous flow conditions, where some synthetic steps that were not permitted for safety reasons can be performed with minimum risk. In this review we focused our attention only on very recent advances in the continuous flow multistep synthesis of organic molecules which found application as APIs, especially highlighting the contributions described in the literature from 2013 to 2015, including very recent examples not reported in any published review. Without claiming to be complete, we will give a general overview of different approaches, technologies, and synthetic strategies used so far, thus hoping to contribute to minimize the gap between academic research and pharmaceutical manufacturing. A general outlook about a quite young and relatively unexplored field of research, like stereoselective organocatalysis under flow conditions, will be also presented, and most significant examples will be described; our purpose is to illustrate all of the potentialities of continuous flow organocatalysis and offer a starting point to develop new methodologies for the synthesis of chiral drugs. Finally, some considerations on the perspectives and the possible, expected developments in the field are briefly discussed.
The reduction of the nitro group represents a powerful and widely used transformation that allows to introducing an amino group in the molecule. New synthetic strategies for complex functionalized ...molecular architectures are deeply needed, including highly efficient and selective nitro reduction methods, tolerant of a diverse array of functional moieties and protecting groups. Since chiral amino groups are ubiquitous in a variety of bioactive molecules such as alkaloids, natural products, drugs, and medical agents, the development of reliable catalytic methodologies for the nitro group reduction is attracting an increasing interest also in the preparation of enantiomerically pure amines. In this context, the modern reduction methods should be chemoselective and respectful of the stereochemical integrity of the stereogenic elements of the molecule. The review will offer an overview of the different possible methodologies available for this fundamental transformation, with special attention on the most recent contributions in the field, especially in the last ten years: hydrogenations, metal dissolving and hydride transfer reductions, catalytic transfer hydrogenations, and metal-free reductions. The main advantages or limitations for the proposed methods will be briefly discussed, highlighting in some cases the most important features of the presented reduction methodologies from an industrial point of view.
A new, mild, metal-free, HSiCl3-mediated reduction of both aromatic and aliphatic nitro groups to amines that is of wide general applicability, tolerant of many functional groups, and respectful of ...the stereochemical integrity of stereocenters is reported.
Coypu (Myocastor coypus) as a meat resource: heterotic and maternal effects on growth traits Spiaggi, E.P; Benaglia, A; Masso, R.J. di (Centro de Estudios Ambientales de Veterinaria (CEAV), Catedra de Genetica y Biometria, Consejo de Investigaciones, Facultad de Ciencias Veterinarias, Universidad Nacional de Rosario Ov. Lagos y Ruta 33, 2170 Casilda (Argentina))
Animal Science (United Kingdom),
(1998), Letnik:
68, Številka:
4
Publication
Objective To evaluate serum antimüllerian hormone (AMH) level modification after surgical excision of ovarian endometriomas. Design Systematic review. MEDLINE search from January 1990 to April 2012 ...using the combination of medical terms endometriosis, endometrioma, endometriotic cyst, and AMH or antimüllerian hormone, MIF or müllerian inhibiting factor. Reference lists of selected studies were checked for additional potential contributions. Setting Not applicable. Patient(s) Women with ovarian endometriomas requiring surgery. Intervention(s) Serum AMH level assessment. Main Outcome Measure(s) Serum AMH level modifications. Result(s) Eleven articles satisfied our selection criteria. Data pooling were deemed inopportune owing to the heterogeneity of the study designs and of the reported parameters. Nine of 11 studies documented a statistically significant reduction of serum AMH level after surgery. The two studies failing to document this decrease were published by the same study group and partly overlapped. The magnitude of the decline was more evident in women operated on for bilateral endometriomas. Conclusion(s) Evidence deriving from the evaluation of serum AMH level modifications after surgical excision of endometriomas supports a surgery-related damage to ovarian reserve.
Celebrating Franco Cozzi's 70 th Birthday Benaglia, Maurizio; Gennari, Cesare
European journal of organic chemistry,
August 6, 2021, Letnik:
2021, Številka:
29
Journal Article
Recenzirano
Odprti dostop
On the occasion of the 70th birthday of Franco Cozzi (Università degli Studi di Milano), a selection of articles by his friends, colleagues, and former students, who are among the leading researchers ...in the field of Organic Chemistry in Italy, Europe, and overseas, covering the entire spectrum of synthetic organic, bioorganic, physical‐organic chemistry and organic stereochemistry, is presented.
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