3,5-Difluorophenyl-alpha-hydroxy-alpha-methylacetic acid → 3-[N'-(3,5-difluorophenyl-alpha-hydroxy-alpha-methylacetyl)-L-alaninyl]-amino-2,3-dihydro-1-methyl-5-(2-fluorophenyl)-1H-1,4-Benzodiazepin-2-one

Participants

Reaction Steps

Following General Procedure D above using 3,5-difluorophenyl-α-hydroxy-α-methylacetic acid and 3-(L-alaninyl)-amino-2,3-dihydro-1-methyl-5-(2-fluorophenyl)-1H-1,4-Benzodiazepin-2-one (Example 8-b), the title compound was prepared. 1H NMR (CDCl3, 300 MHz) δ=1.43 (3H, d, J=7.1 Hz), 1.79 (3H, s), 3.47 (3H, s), 4.15 (1H, s), 4.58 (1H, p, J=7.3 Hz), 5.45 (1H, d, J=8.0 Hz), 6.70 (1H, m), 7.14-7.27 (3H, m), 7.32-7.47 (6H, m), 7.55-7.63 (3H, m), 7.78 (1H, d, J=7.8 Hz). HRMS calc for C28H27N4O4F2 521.2000 (MH+), Found: 521.2.

Provenance & Evidence