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A mixture of 2-chloropyrimidine (1.02 g, 8.9 mmol) and ethylendiamine (15 mL) was refluxedfor 2 h. The mixture was diluted with brine and extracted with DCM. The solvent was removedunder reduced pressure. The crude product was purified by flash chromatography (DCM: CH3OH=7: 1) to give a yellow oil ( 700 mg, yield 57%).
Preparation of N-(2-Pyrimidinyl)ethylenediamine a)N-Boc-N'-(2-Pyrimidinyl)ethylenediamine N-(Boc)ethylenediamine (0.80 g, 5.0 mmol) (Syn. Commun. 1990, 20, 255-264) was dissolved in 1-propanol (12 mL) and treated with K2 CO3 (1.2 g, 9.0 mmol), followed by 2-chloropyrimidine (0.91 g, 8.0 mmol), and the mixture was heated to reflux for 24 h. The reaction mixture was poured into H2 O (30 mL) and extracted with EtOAc (3*30 mL). The combined organic fractions were dried (MgSO4) and concentrated to give the title compound as a yellow solid (1.6 g): MS (ES) m/e 238.9 [M+H]+.
2-(5,11-dioxo-6a,11-dihydroisoindolo[2,1-a]quinazolin-6(5H)-yl)acetic acid[ No CAS ]
[ 137583-05-2 ]
2-(5,11-dioxo-6a,11-dihydroisoindolo[2,1-a]quinazolin-6(5H)-yl)-N-(2-(pyrimidin-2-ylamino)ethyl)acetamide[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
85%
A mixture of 2-(5,11-dioxo-6a,11-dihydroisoindolo[2,1-a]quinazolin-6(5H)-yl)acetic acid (X_10,38 mg, 0.12 mmol), HATU (26.7 mg, 0.07 mmol) and N,N-Diisopropylethylamine (15.1 mg, 0.12mmol) in 2 ml of DCM was stirred for 30 min at room temperature. Then N1-(pyrimidin-2-yl)ethane-1,2-diamine (X_7, 8.1 mg, 0.06 mmol) was added, the mixture was stirred 2 h at room temperature.After removal of solvent under reduced pressure. The crude product was purified by flashchromatography (EA: PE = 1: 5) to give compound 9 as a white solid (45 mg, yield 85%).
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