01253nas a2200181   4500008004100000022001400041245011300055210006900168260000900237300001400246490000700260520058900267100002300856700002400879700002300903700002100926856012400947       2024                        eng d  a1523-706000aHighly stereoselective diels-alder-based strategy for the synthesis of 3-epi-formicin A and 1-epi-formicin B0 aHighly stereoselective dielsalderbased strategy for the synthesi  cAPR   a3961-39650 v263 a<p>
	The first enantioselective approach based on a highly stereoselective Diels-Alder reaction for the synthesis of 3-epi-formicin A and 1-epi-formicin B with rare N-acetylcysteamine-containing indenone thioesters is reported. The strategy utilizes a key Diels-Alder reaction to form the core hydrindane system with three contiguous stereocenters in very high levels of diastereo- and regioselectivity and one-pot oxidation/isomerization/dehydrogenation. The scope of this method was tested with different substrates to give cycloadducts in a highly diastereoselective manner.</p>
1 aKhamkar, Sunil, L.1 aHandore, Kishor, L.1 aShinde, Harish, M.1 aReddy, Srinivasa  uhttps://library.ncl.res.in/content/highly-stereoselective-diels-alder-based-strategy-synthesis-3-epi-formicin-and-1-epi02016nas a2200217   4500008004100000022001400041245013300055210006900188260000800257300000800265490000600273520124400279100002301523700001801546700001701564700002301581700002401604700001901628700002101647856013001668       2025                        eng d  a2399-366900aScalable and sustainable reductive amidation of nitroarenes, nitroalkenes, and nitroalkyls with acyl saccharins in aqueous media0 aScalable and sustainable reductive amidation of nitroarenes nitr  cJUN  a1840 v83 a<p>
	Amide bond formation is essential in both organic and medicinal chemistry, however, most existing methods present poor ecological efficiency. Here, we report a scalable and sustainable method for synthesizing N-substituted amides from nitroarenes, nitroalkenes, nitroalkyls, and acyl saccharin in aqueous media. This atom-efficient approach avoids column chromatography, offers high yield, and is compatible with various functional groups. It is applicable to synthesize Dispyrin, a bromopyrrole alkaloid, amide-based drugs, and agrochemicals, including paracetamol, with solvent and saccharin recycling. A comprehensive Life Cycle Assessment (LCA; ISO 14044) was conducted to evaluate the environmental impacts and sustainability of nine Active Pharmaceutical Ingredients (APIs) produced via Amidation Route (AR) and Saccharin Amidation Route (SAR). The study shows SAR methods reduce carbon footprints and environmental impacts compared to AR methods, being carbon-negative and resource-efficient. Additional reductions can be achieved through saccharin recycling and the integration of renewable energy sources, demonstrating saccharin-based processes potential to minimize environmental burdens in pharmaceutical synthesis.</p>
1 aKhamkar, Sunil, L.1 aMohan, Rayala1 aSanthosh, J.1 aShinde, Harish, M.1 aHandore, Kishor, L.1 aMohan, Venkata1 aReddy, Srinivasa  uhttps://library.ncl.res.in/content/scalable-and-sustainable-reductive-amidation-nitroarenes-nitroalkenes-and-nitroalkyls-acyl