C(O)C.C(O)(=O)C.C[O:9][C:10](=O)[CH:11]([CH3:27])[CH2:12][N:13]([C:19]1[C:24]([NH2:25])=[CH:23][N:22]=[C:21]([Cl:26])[N:20]=1)[CH:14]1[CH2:18][CH2:17][CH2:16][CH2:15]1>CCOCC>[Cl:26][C:21]1[N:22]=[CH:23][C:24]2[NH:25][C:10](=[O:9])[CH:11]([CH3:27])[CH2:12][N:13]([CH:14]3[CH2:18][CH2:17][CH2:16][CH2:15]3)[C:19]=2[N:20]=1A mixture of 1500 mL of ethanol, 25 mL of acetic acid and 35.2 g of the (rac)-3-[(5-amino-2-chloro-pyrimidin-4-yl)-cyclopentyl-amino]-2-methyl-propanoic acid methyl ester (V-1) prepared in the previous step was heated at reflux overnight, and then concentrated under reduced pressure. The residue was taken up in dichloromethane and washed successively with 10% sodium bicarbonate solution, and then water and dried over anhydrous sodium sulfate. The mixture was filtered and then concentrated under reduced pressure to give 31 g of the crude product. Trituration of the residue with ether, provided 20.7 g of (rac)-2-chloro-9-cyclopentyl-7-methyl-5,7,8,9-tetrahydro-pyrimido[4,5-b][1,4]diazepin-6-one (VI-1).
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