Triethylamine → Pyrimidine-5-carboxylic acid(1-{1-[4-(4-difluoromethoxy-phenoxy)-phenyl]-ethylcarbamoyl}-cyclopropyl)-amide

376 μL (2.70 mmol) of triethylamine and 0.52 g (1.62 mmol) of TBTU were added to a solution of 0.28 g (1.35 mmol) of 1-[(pyrimidin-5-carbonyl)-amino]-cyclo-propanecarboxylic acid (from 1b) in 5 mL DMF and the mixture was stirred for 5 min at RT. Then 0.42 g (1.50 mmol) of 1-[4-(4-difluoromethoxy-phenoxy)-phenyl]-ethylamine was added and the mixture was stirred for 30 min at ambient temperature. The reaction mixture was purified by chromatography (reversed phase). The acetonitrile was distilled off, the aqueous phase was made basic with ammonia and extracted with dichloromethane. The organic phase was dried and evaporated down.

1. stirringthe mixture was stirred for 30 min at ambient temperature
2. customThe reaction mixture was purified by chromatography (reversed phase)
3. distillationThe acetonitrile was distilled off
4. extractionextracted with dichloromethane
5. customThe organic phase was dried
6. customevaporated down

ORD-Eintrag

ord-1b7f1da8d8be4e94af0db65b7be0cebc

Quelldatensatz

uspto-grants-2014_12

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US08916589B2