Реакция #1135863

Уравнение реакции

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

Выход 50.0%

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

Выход 50.0%

Растворители

dichloromethane

Условия реакции

Обработка

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

Методика

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.

Источник