Cesium carbonate → 1-[(2S)-1,4-Dioxan-2-ylmethyl]-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (2.5 g) was added to a suspension of cesium carbonate (2.50 g) in 1,4-dioxane (30 ml). After stirring, (2R)-1,4-dioxan-2-ylmethyl methanesulfonate (2.78 g) was added and the mixture was stirred at 90° C. for four hours. After leaving to cool, the reaction solution was filtered, and the filtrate was concentrated. The residue was purified by silica gel column chromatography [chloroform:methanol=19:1 (v/v)] to give 3.79 g of the title compound.

1. stirringthe mixture was stirred at 90° C. for four hours
2. customAfter leaving
3. temperatureto cool
4. filtrationthe reaction solution was filtered
5. concentrationthe filtrate was concentrated
6. customThe residue was purified by silica gel column chromatography [chloroform:methanol=19:1 (v/v)]

ORD-Eintrag

ord-d556cfaa76c244e19fd60fcfdf54ce32

Quelldatensatz

uspto-grants-2015_01

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US08933103B2