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ChemicalBook CAS DataBase List N-BOC-(R)-1-AMINO-2-PROPANOL
119768-44-4

N-BOC-(R)-1-AMINO-2-PROPANOL synthesis

3synthesis methods
-

Yield:119768-44-4 100%

Reaction Conditions:

in dichloromethane at 0 - 20; for 2 h;Inert atmosphere;

Steps:

Intermediate 3 (1-3) (2i?-Hydroxy-propyl)-carbamic acid tert- vXy\ ester (1-3)
Intermediate 3 (1-3) (2i?-Hydroxy-propyl)-carbamic acid tert- vXy ester (1-3) Di-fert-butyl dicarbonate (58.1 g, 266.3 mmol) in DCM (50 mL) was added to a stirred solution of (i?)-(-)-l-amino-2-propanol in DCM (50 mL) at 0 °C under nitrogen. The mixture was stirred at rt for 2 h. The mixture was diluted with cooled water and extracted with DCM. The organic layer was separated, dried (Na2S04), filtered and the solvents evaporated in vacuo to yield intermediate 1-3 as a colorless oil (47 g, quant.). The product was used in the next step without further purification.

References:

JANSSEN PHARMACEUTICA NV;VAN GOOL, Michiel, Luc, Maria;ALONSO-DE DIEGO, Sergio-Alvar;CID-Nú?EZ, José, Maria;DELGADO-GONZáLEZ, óscar;DECORTE, Annelies, Marie, Antonius;MACDONALD, Gregor, James;MEGENS, Antonius, Adrianus, Hendrikus, Petrus;TRABANCO-SUáREZ, Andrés, Avelino;GARCíA-MOLINA, Aránzazu;ANDRéS-GIL, José, Ignacio WO2014/195311, 2014, A1 Location in patent:Page/Page column 78

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