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• W2321365024 abstract "A manufacturing route for the synthesis of raltegravir potassium 1 was developed via a thermal rearrangement of amidoxime DMAD adducts 6 to construct the key, highly functionalized hydroxypyrimidinone core 7. Utilizing this route 1 was prepared in nine linear chemical steps with 22% overall yield. A second-generation synthesis was subsequently developed that solved the key chemical, productivity, and environmental impact issues of the initial synthesis. Highlights of the new synthesis include a highly selective methylation, 3−4-fold higher productivity, and a 65% reduction of combined organic and aqueous waste produced. The efficient second-generation manufacturing route provides raltegravir potassium 1 in 35% overall yield." @default.
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• W2321365024 date "2010-11-16" @default.
• W2321365024 modified "2023-10-14" @default.
• W2321365024 title "Development of a Second-Generation, Highly Efficient Manufacturing Route for the HIV Integrase Inhibitor Raltegravir Potassium" @default.
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• W2321365024 doi "https://doi.org/10.1021/op100257r" @default.
• W2321365024 hasPublicationYear "2010" @default.
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