2,4-DIMETHOXYPYRIMIDINE-6-CARBOXYLIC ACID

Oxalyl chloride (0.092 mL, 1.05 1 mmol) was added dropwise to a stirred mixture of 2, 6- dimethoxypyrimidine-4-carboxylic acid (168 mg, 0.910 mmol) and catalytic N, N-dimethylformamide (5.42 pL, 0.070 mmol) in dichloromethane (14 mL). After stirring for 2.3 hours, volatiles were removed under reduced pressure to give a white solid. The solid was treated with t-butyl methyl ether. Any insolubles were removed by filtration and the filtrate was concentrated under reduced pressure (bath temperature: 25 C) to give the titled compound that was dissolved in CH2C12 (10 mL).Example 43 Preparation of (S)-3-[(2, 6-dimethoxy-pyrimidine-4-carbonyl)-amino]-2-{[5-(3-hydroxy-benzylcarbamoyl)-3-methyl-thiophene-2-carbonyl]-amino}-propionic acid (S)-3-amino-2-{[5-(3-hydroxy-benzylcarbamoyl)-3-methyl-thiophene-2-carbonyl]-amino}-propionic acid methyl ester (HCl salt) (100 mg, 0.23 mmol) was dissolved in DMF (2.5 ml) and the following reagents were successively added at rt:

Molecular Weight:184.15
XLogP3:0.7
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:3
Exact Mass:184.04840674
Monoisotopic Mass:184.04840674
Topological Polar Surface Area:81.5
Heavy Atom Count:13
Complexity:187
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes