Humphrey, Guy R. published the artcileDevelopment of a Second-Generation, Highly Efficient Manufacturing Route for the HIV Integrase Inhibitor Raltegravir Potassium, HPLC of Formula: 519028-33-2, the main research area is Raltegravir Potassium preparation scaleup methylation amidoxime rearrangement green chem.
A manufacturing route for the synthesis of Raltegravir Potassium was developed via thermal rearrangement of amidoxime DMAD adducts to construct the key, highly functionalized hydroxypyrimidinone core, 2-(1-benzyloxycarbonylamino-1-methylethyl)-5,6-dihydroxypyrimidine-4-carboxylic acid Me ester. Utilizing this route, Raltegravir Potassium was prepared in nine linear chem. steps with 22% overall yield. A second-generation synthesis was subsequently developed that solved the key chem., 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 in 35% overall yield.
Organic Process Research & Development published new progress about Green chemistry. 519028-33-2 belongs to class pyrimidines, name is Benzyl (2-(4-((4-fluorobenzyl)carbamoyl)-5-hydroxy-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)carbamate, and the molecular formula is C23H23FN4O5, HPLC of Formula: 519028-33-2.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia