1,2-Dichloroethane → 2,2-Dimethyl-N-[1-[6-(5-{2-[4-(trifluoromethyl)phenyl]ethyl}-1,2,4-oxadiazol-3-yl)quinolin-2-yl]pyrrolidin-3-yl}propanamide

To a mixture of the product of Step E, (66 mg) in anhydrous diglyme (2 mL) was added 4-trifluoromethylphenylpropionic acid (1.1 eq.) and EDC (2 eq.). The reaction mixture was heated to 50° C. overnight. After approximately 18 h, the mixture was heated at 110° C. for 2 hr. The mixture was cooled to r.t., quenched with water and extracted with excess EtOAc. The combined extracts were dried over a drying agent filtered and the solvent removed under vacuum. The residue was purified by preparative TLC eluting with EtOAc to afford the product, MS: m/z 538.

1. temperaturethe mixture was heated at 110° C. for 2 hr
2. temperatureThe mixture was cooled to r.t.
3. customquenched with water
4. extractionextracted with excess EtOAc
5. customThe combined extracts were dried over a drying agent
6. filtrationfiltered
7. customthe solvent removed under vacuum
8. customThe residue was purified by preparative TLC
9. washeluting with EtOAc
10. customto afford the product, MS

ORDレコード

ord-5b2ee72421e84c96a53e63a90b2cd355

出典データセット

uspto-grants-2006_08

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US07084156B2