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ChemicalBook CAS DataBase List 4-IODOTETRAHYDRO-2H-PYRAN
25637-18-7

4-IODOTETRAHYDRO-2H-PYRAN synthesis

3synthesis methods
-

Yield:25637-18-7 64.3%

Reaction Conditions:

with 1H-imidazole;iodine;triphenylphosphine in tetrahydrofuran at 0 - 20;

Steps:

Step 1: 4-iodotetrahydro-2H-pyran
A RBF was charged with tetrahydro-2H-pyran-4-ol (2.0 g, 19.58 mmol), imidazole (1.600 g, 23.50 mmol), triphenylphosphine (5.39 g, 20.56 mmol), and tetrahydrofuran (39.2 ml) and cooled to 0° C. A solution of iodine (5.96 g, 23.50 mmol) in tetrahydrofuran (39.2 ml) was added slowly dropwise.
The reaction was warmed to room temperature and stirred overnight.
The reaction was diluted with ethyl acetate and washed with water.
The aqueous layer was extracted with ethyl acetate, and the combined organic layers were dried with sodium sulfate, filtered, and concentrated.
The material was purified via column chromatography (RediSep Gold 80 g, gradient elution 0-50% EtOAc:Heptane) to afford 4-iodotetrahydro-2H-pyran (2.67 g, 12.59 mmol, 64.3% yield) as a clear light yellow oil.

References:

Amgen Inc.;Weiss, Matthew;Boezio, Alessandro;Boezio, Christiane;Butler, John R.;Chu-Moyer, Margaret Yuhua;Dimauro, Erin F.;Dineen, Thomas;Graceffa, Russell;Guzman-Perez, Angel;Huang, Hongbing;Kreiman, Charles;La, Daniel;Marx, Isaac E.;Milgrim, Benjamin Charles;Nguyen, Hanh Nho;Peterson, Emily;Romero, Karina;Sparling, Brian US9212182, 2015, B2 Location in patent:Page/Page column 79

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