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METHYL (S)-3-BOC-AMINOBUTYRATE synthesis

9synthesis methods
-

Yield:106539-14-4 99%

Reaction Conditions:

at 20; for 18 h;

Steps:

146.1

Example 146.2-Cyclopropyl-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid ((S)-3-methanesulfonyl-l ,2,2- trimethyl-propyl) amideStep 1(S)-3-(tert-Butoxycarbonylamino)butanoic acid (1.0 g, 4.9 mmol) was dissolved in toluene (38 mL) and methanol (11 mL). The solution was cooled in an ice/water bath andtrimethylsilyl diazomethane (2 M solution in hexanes, 12.3 mL, 24.6 mmol) was added slowly. The reaction was stirred at 20°C for 18 h then concentrated. The residue was absorbed on to silica gel and purified by silica gel chromatography (ethyl acetate/hexanes) to give 1.06 g (99%) of (S)-3-tert-butoxycarbonylamino-butyric acid methyl ester.

References:

WO2011/144585,2011,A1 Location in patent:Page/Page column 214

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