Piperazine-2,6-dione

To a stirred solution of [0447] To a stirred solution of A mixture of (S) -5- (1- ( (tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4- (difluoromethoxy) phenyl) oxazole-4-carboxylic acid (250 mg, 0.53 mmol) , piperazine-2, 6-dione (73 mg, 0.64 mmol) , EDCI (153 mg, 0.80 mmol) and HOAT (182 mg, 1.33 mmol) in DCM (15 mL) was stirred at 0, and DIPEA (0.37 mL, 2.14 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 10 h and washed with water (10 mL × 2) . The organic layer was dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluted with DCM/MeOH (v/v) 60/1 to give the title compound as a light yellow solid (156 mg, 51) .1H NMR (400 MHz, CDCl3) : delta ppm 7.59 (dd, J1 8.3 Hz, J2 1.7 Hz, 1H) , 7.56 (d, J 1.6 Hz, 1H) , 7.25 (d, J 8.2 Hz, 1H) , 6.71 (t, JF-H 75.0 Hz, 1H) , 5.32-5.25 (m, 1H) , 5.01 (br. s, 2H) , 4.63 (br. s, 2H) , 3.98 (d, J 6.9 Hz, 2H) , 1.54 (d, J 7.0 Hz, 3H) , 1.40 (s, 9H) , 1.33-1.29 (m, 1H) , 0.71-0.66 (m, 2H) , 0.43-0.39 (m, 2H) and MS-ESI: m/z 465.2 [M+H-100] +.The compound (S) -5- (1 - ((tert-butoxycarbonyl) amino) ethyl) -2- (3- (cyclopropylmethoxy) -4-(difluoromethoxy) phenyl ) -oxazole-4-carboxylic Acid (250mg, 0.53mmol), Step 2 4-[(4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4, 5-dihydro-1, 2-oxazol-3-yl]-2-methylphenyl)carbonyl]

Molecular Weight:114.10
XLogP3:-1.3
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:3
Exact Mass:114.042927438
Monoisotopic Mass:114.042927438
Topological Polar Surface Area:58.2
Heavy Atom Count:8
Complexity:118
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes