Réaction #85892

Équation de réaction

tert-butyl 5-((7-chloropyrido[4,3-b]pyrazin-5-ylamino)methyl)-3,3-difluoropiperidine-1-carboxylate

4-morpholinophenylboronic acid

tri(cyclohexyl)phosphine

Cs2CO3

→

title compound

tert-butyl 3,3-difluoro-5-((7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)piperidine-1-carboxylate

Solvants

dimethoxyethane H2O

Conditions de réaction

Traitement

1. 1
   Autrewas sealed in a microwave reaction tube
2. 2
   TempératureThe mixture was cooled to room temperature
3. 3
   Concentrationconcentrated under reduced pressure
4. 4
   Autrethe residue was purified by chromatography

Mode opératoire

A mixture of tert-butyl 5-((7-chloropyrido[4,3-b]pyrazin-5-ylamino)methyl)-3,3-difluoropiperidine-1-carboxylate (206 mg, 0.5 mmol), 4-morpholinophenylboronic acid (207 mg, 1.0 mmol), tri(cyclohexyl)phosphine (56 mg, 0.2 mmol), Pd2(dba)3 (91 mg, 0.1 mmol) and Cs2CO3 (325 mg, 2.0 mmol) in dimethoxyethane/H2O was sealed in a microwave reaction tube and stirred at 160° C. for 80 minutes in a microwave reactor. The mixture was cooled to room temperature, concentrated under reduced pressure, and the residue was purified by chromatography to give the title compound. MS (m/z): 541 (M+H)+.

Source