Dicyclohexylcarbodiimide → 2-{2-[2-(4-Hydroxy-phenoxy)-acetoxy]-acetylamino}-3-(4-hydroxy-phenyl)-propionic acid methyl ester

To a solution of (4-hydroxy-phenoxy)-acetic acid 12 (10 grams, 59.52 mmol) and 2-(2-hydroxy-acetylamino)-3-(4-hydroxy-phenyl)-propionic acid methyl ester 3 (15 grams, 59.28 mmol) in anhydrous dichloro methane (100 mL) under an nitrogen atmosphere at 0° C. is added to a solution of 1,3-dicyclohexyl carbodiimide (31 grams, 150.24 mmol) in dichloro methane (75 mL) drop wise. Later it is stirred at room temperature for 6 hours. The solids are filtered off. The organic phase is washed with 5% sodium bicarbonate (2×25 mL) and water (2×25 mL), dried over sodium sulphate, and distilled to give crude 13, which can be purified in appropriate solvent.

1. filtrationThe solids are filtered off
2. washThe organic phase is washed with 5% sodium bicarbonate (2×25 mL) and water (2×25 mL)
3. dry with materialdried over sodium sulphate
4. distillationdistilled
5. customto give crude 13, which
6. customcan be purified in appropriate solvent

ORD-Eintrag

ord-098ae06b09584bebaf73a40cce664ac1

Quelldatensatz

uspto-grants-2011_05

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US07935843B2