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3-(PyriMidin-2-ylaMino)-pyrrolidine-1-carboxylic acid tert-butyl ester synthesis

1synthesis methods
1722-12-9 Synthesis
2-Chloropyrimidine

1722-12-9
541 suppliers
$10.00/1g

186550-13-0 Synthesis
tert-Butyl 3-aminopyrrolidine-1-carboxylate

186550-13-0
223 suppliers
$8.00/1g

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Yield:950649-08-8 74%

Reaction Conditions:

with N-ethyl-N,N-diisopropylamine in isopropyl alcohol; for 72 h;Heating / reflux;

Steps:

42.A

Step A: tert-Butyl 3-(pyrimidine-2-ylamino)- 1 -pyrrolidinecarboxylateTo a solution of l-N-Boc-3-amino-pyrrolidone (4.00 g, 21.5 mmol) in isopropanol (50 mL) is added 2-chloropyrimidine (2.94 g, 25.8 mmol) and diisopropylethylamine (4.16 g, 32.3 mmol). The mixture is heated at reflux for 3 days, allowed to come to room temperature, evaporated in vacuo and purified on silica gel using ethyl acetate/heptane to give the desired product (4.20 g, 74%).

References:

WO2007/106705,2007,A1 Location in patent:Page/Page column 101-102