반응 #168017

반응 방정식

4-chloro-6-(5-isopropyl-2-methylphenyl)-2-(3-methyl-1-tosyl-1H-indol-4-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine

(R)-tert-butyl 3-methylpiperazine-1-carboxylate

DIEA

→

title compound

(R)-tert-Butyl 4-(6-(5-isopropyl-2-methylphenyl)-2-(3-methyl-1-tosyl-1H-indol-4-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)-3-methylpiperazine-1-carboxylate

용매

N,N-dimethylacetamide

EtOAc

반응 조건

후처리

1. 1
   기타Reaction mixture
2. 2
   세척washed with sat aq NaHCO3 and brine
3. 3
   건조The organic layer was then dried over Na2SO4
4. 4
   농축concentrated
5. 5
   기타purified via FCC (0-40% EtOAc/heptane)

실험 절차

A mixture of 4-chloro-6-(5-isopropyl-2-methylphenyl)-2-(3-methyl-1-tosyl-1H-indol-4-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine (Example 17-E) (0.274 g, 0.468 mmol), (R)-tert-butyl 3-methylpiperazine-1-carboxylate (0.375 g, 1.87 mmol) and DIEA (0.33 mL, 1.87 mmol) in N,N-dimethylacetamide (3 mL) was heated at 125° C. for 15 h. Reaction mixture was diluted with EtOAc, washed with sat aq NaHCO3 and brine. The organic layer was then dried over Na2SO4, concentrated, purified via FCC (0-40% EtOAc/heptane) to provide the title compound. MS (ESI+) m/z 749.4 (M+H)+.

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