3-(Difluoromethyl)-[1,2,4]triazolo[4,3-a]pyrazine → 3-(difluoromethyl)-5H,6H,7H,8H-(1,2,4)triazolo(4,3-a)pyrazine

3-(Difluoromethyl)-[1,2,4]triazolo[4,3-a]pyrazine 23c (460 mg, 2.70 mmol) was dissolved in 10 mL of methanol, followed by addition of Pd—C (10%, 46 mg), and the reactor was purged with hydrogen for three times. After stirring for 3 hours, the reaction mixture was filtered and the filter cake was washed with methanol (10 mL). The filtrate was concentrated under reduced pressure to obtain crude 3-(difluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine 23d (400 mg) as a light yellow oil. The product was used directly in the next reaction without purification.

1. customthe reactor was purged with hydrogen for three times
2. filtrationthe reaction mixture was filtered
3. washthe filter cake was washed with methanol (10 mL)
4. concentrationThe filtrate was concentrated under reduced pressure

ORD-Eintrag

ord-6cf3853937064690aacf7b2cc61367e4

Quelldatensatz

uspto-grants-2016_03

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US09273052B2