4-(5-AMINO-6-CHLORO-4-PYRIMIDINYL)-1-PIPERAZINECARBOXYLIC ACID 1,1-DIMETHYLETHYL ESTER synthesis
- Product Name:4-(5-AMINO-6-CHLORO-4-PYRIMIDINYL)-1-PIPERAZINECARBOXYLIC ACID 1,1-DIMETHYLETHYL ESTER
- CAS Number:853679-43-3
- Molecular formula:C13H20ClN5O2
- Molecular Weight:313.78
Yield:853679-43-3 99%
Reaction Conditions:
in triethylamine;toluene; for 12 h;Heating / reflux;
Steps:
26.1
To a solution of 4, 6-dichloro-5-aminopyrimidine (1 g, 6. 1 mmol) in TEA (2 mL) and toluene (10 mL) was added 1-Boc-piperazine (2.3 g, 12.3 mmol). The mixture was refluxed for 12 hours. The solvent was removed and the residue was subject to chromatography on silica gel to afford the product 4- (5-amino-6-chloropyrimidin-4-yl)- piperazine-l-carboxylic acid tert-butyl ester (1.9g, 99%). 1H NMR (CDC13, 400 Hz) 8 8.16 (s, 1H), 3.87 (s, 2H), 3.56 (m, 4H), 3.29 (m, 4H), 1.49 (s, 9H). MS (ESI+) [M+H] + 314.
References:
WO2005/51304,2005,A2 Location in patent:Page/Page column 68-69