New Manufacturing Route to Picoxystrobin

A new and efficient manufacturing technology is disclosed in the present work for the preparation of picoxystrobin in which all of the intermediates can be used directly in the next step of the process without purification

A Facile, Six-Step Process for the Synthesis of (3<i>S</i>,5<i>S</i>)‑3-Isopropyl-5-((2<i>S</i>,4<i>S</i>)‑4-isopropyl-5-oxo-tetrahydrofuran-2-yl)-2-oxopyrrolidine-1-carboxylic Acid <i>tert</i>-Butyl Ester, The Key Synthetic Intermediate of Aliskiren

A facile, six-step process for the synthesis of (3<i>S</i>,5<i>S</i>)-3-isopropyl-5-((2<i>S</i>,4<i>S</i>)-4-isopropyl-5-oxotetrahydro- furan-2-yl)-2-oxopyrrolidine-1-carboxylic acid <i>tert</i>-butyl ester from (<i>S</i>)-4-benzyloxazolidin-2-one <b>2</b> in an overall 50% yield is reported. The key transformations include: a highly efficient diastereoselective epoxidation, Lewis acid-catalyzed ring-opening with bromide, an S_N2 reaction using NaN₃, and a tandem reduction–cyclization reaction

Efficient Synthesis of 3-<i>R</i>-Boc-amino-4-(2,4,5-trifluorophenyl)butyric Acid

<div><p></p><p>3-<i>R</i>-Boc-amino-4-(2,4,5-trifluorophenyl)butyric acid (<b>9</b>) was obtained from <i>L</i>-methionine in six steps with a total yield of 32%. The α-amino acid segment of <i>L</i>-methionine was transferred to chiral aziridine by amino protection, reduction, hydroxyl derivation, and cyclization. After ring opening of 2,4,5-trifluoro-phenyl magnesium bromide, the methylthiomethyl group was then hydrolyzed to β-amino alcohol and oxidized to the target β-amino acid.</p></div