Methanol → (4-{2-[(1S,2R)-2-{1-[5-(ethoxymethyl)pyrimidin-2-yl]piperidin-4-yl}cyclopropyl]ethoxy}-2-fluorophenyl)acetic acid

Methyl (4-{2-[(1S,2R)-2-{1-[5-(ethoxymethyl)pyrimidin-2-yl]piperidin-4-yl}cyclopropyl]ethoxy}-2-fluorophenyl)acetate (1.4 g, 2.97 mmol) was dissolved in THF (3 ml):MeOH (30 ml) and 1M lithium hydroxide (14.84 ml, 14.84 mmol) added. The mixture was stirred at RT overnight. The mixture was concentrated in vacuo and the residue diluted with water (5 mL). The pH of the solution was adjusted to pH˜5 by addition of 1N HCl and the aqueous phase was extracted with EtOAc (3×10 mL). The organic fractions were combined, washed with brine, dried over MgSO4 and concentrated under reduced pressure to afford the title compound. LC/MS (m/z): 458 (M+H)+.

1. concentrationThe mixture was concentrated in vacuo
2. additionthe residue diluted with water (5 mL)
3. additionThe pH of the solution was adjusted to pH˜5 by addition of 1N HCl
4. extractionthe aqueous phase was extracted with EtOAc (3×10 mL)
5. washwashed with brine
6. dry with materialdried over MgSO4
7. concentrationconcentrated under reduced pressure

ORDレコード

ord-894090eea6d44192ae50201907d83998

出典データセット

uspto-grants-2015_04

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US09018224B2