Hydrochloric Acid → 2-(4-Chloro-1,6-dihydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-3-yl)acetic acid

To a solution of ethyl 2-(4-chloro-1-hydroxy-6-isopropoxy-1,3-dihydrobenzo[c][1,2]oxaborol-3-yl)acetate (200 mg, 0.74 mmol) in 10 mL THF was added LiOH (100 mg, 2.22 mmol) in 5 mL H2O dropwise at 0° C. The mixture was stirred at room temperature for 1.5 h and acidified to pH=5.0 using 1N HCl (8 mL). The resulting mixture was extracted with EtOAc (3×10 mL). The combined organic layers were dried over anhydrous Na2SO4 and concentrated in vacuo. The residue was use directly in next step reaction without further purification.

1. extractionThe resulting mixture was extracted with EtOAc (3×10 mL)
2. dry with materialThe combined organic layers were dried over anhydrous Na2SO4
3. concentrationconcentrated in vacuo
4. customdirectly in next step reaction
5. customwithout further purification

ORD-Eintrag

ord-b3641fc48f274c869139882fbe0ce260

Quelldatensatz

uspto-grants-2013_01

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US08343944B2