反应 #1135863

反应方程式

trans-3-{N′-(6-carboxymethoxy-7-oxo-1,6-diaza-bicyclo[3.2.1]octane-2-carbonyl)-hydrazinocarbonyl}-(R)-piperidin-1-carboxylic acid tert-butyl ester

trifluoroacetic acid

→

titled compound

收率 50.0%

trans-{7-oxo-2-[N′—((R)-piperidin-3-carbonyl)-hydrazinocarbonyl]-1,6-diaza-bicyclo[3.2.1]-oct-6-yloxy}-acetic acid

收率 50.0%

溶剂

dichloromethane

反应条件

后处理

1. 1
   workup.STIRRINGThe reaction mixture was stirred for about 1 hour at −10° C.
2. 2
   其他the solvents were evaporated under vacuum
3. 3
   其他to provide a residue
4. 4
   其他The residue was triturated successively with diethyl ether (25 ml) and acetonitrile (25 ml) and solvents
5. 5
   其他were decanted
6. 6
   其他to provide solid
7. 7
   其他that was dried under vacuum

实验过程

To a clear solution of trans-3-{N′-(6-carboxymethoxy-7-oxo-1,6-diaza-bicyclo[3.2.1]octane-2-carbonyl)-hydrazinocarbonyl}-(R)-piperidin-1-carboxylic acid tert-butyl ester (150 mg, 0.32 mmol) in dichloromethane (2 ml) was added trifluoroacetic acid under stirring at −10° C. The reaction mixture was stirred for about 1 hour at −10° C. and the solvents were evaporated under vacuum to provide a residue. The residue was triturated successively with diethyl ether (25 ml) and acetonitrile (25 ml) and solvents were decanted to provide solid that was dried under vacuum to provide 59 mg of titled compound in 50% yield.

来源