Water → 3-{4-[2-(4,5-Dimethyl-thiazol-2-yl)-5,6-dimethyl-pyridin-3-yloxy]-6-methoxy-quinolin-7-yloxy}-propane-1,2-diol

温度

0 °C

4-[2-(4,5-Dimethyl-thiazol-2-yl)-5,6-dimethyl-pyridin-3-yloxy]-6-methoxy-7-oxiranylmethoxy-quinoline (compound 458) (40 mg) was dissolved in methylene chloride (2 ml) to prepare a solution which was then brought to 0° C. Trifluoroacetic acid (0.4 ml) was added thereto, the mixture was stirred at 0° C. for 30 min, and the mixture was then stirred at room temperature for 5 hr. The reaction solution was brought to 0° C., was stirred, and was made alkaline by the addition of a 10% aqueous sodium hydroxide solution. Water was added to the reaction solution, the mixture was extracted with chloroform, and the chloroform layer was then washed with saturated brine and was dried over anhydrous sodium sulfate. The solvent was removed by distillation under the reduced pressure, and the residue was purified by thin layer chromatography using chloroform-methanol to give the title compound (41 mg, yield 100%).

1. customto prepare a solution which
2. customwas then brought to 0° C
3. stirringthe mixture was then stirred at room temperature for 5 hr
4. customwas brought to 0° C.
5. stirringwas stirred
6. extractionthe mixture was extracted with chloroform
7. washthe chloroform layer was then washed with saturated brine
8. dry with materialwas dried over anhydrous sodium sulfate
9. customThe solvent was removed by distillation under the reduced pressure
10. customthe residue was purified by thin layer chromatography

ORDレコード

ord-824fb73ff52c4507a7fa6bdba2425eef

出典データセット

uspto-grants-2009_07

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US07560558B2