Ethanesulfonyl chloride → 6,7-dichloro-4-(3-(4-(ethylsulfonyl)piperazine-1-carbonyl)-4-fluorobenzyl)pyrrolo[1,2-a]pyrazin-1(2H)-one

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Reaction Steps

To a solution of Example 16, P1 in DMF (0.3 M), was added ethanesulfonyl chloride (1 eq) and DIPEA (1 eq). The resulting mixture was stirred for 1 hour at RT. The product was isolated by purification at preparative-HPLC. 1H NMR (400 MHz, DMSO-d6) δ: 10.91 (1H, m, J=5.6 Hz), 7.38-7.18 (3H, m), 7.14 (1H, s), 6.57 (1H, m, J=5.8 Hz), 4.37 (2H, m), 3.87-3.54 (4H, m), 3.31-3.18 (4H, m), 3.05 (2H, q, J=7.41 Hz), 1.21 (3H, t, J=7.20 Hz). MS (ES) C21H21Cl2FN4O4S requires: 514/516, found: 515/517 (M+H)+.

Provenance & Evidence