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2-amino-5-chloro-alpha-methylbenzhydryl alcohol synthesis

4synthesis methods
-

Yield:3158-98-3 530 mg

Reaction Conditions:

in diethyl ether at 0 - 20; for 5 h;Inert atmosphere;

Steps:

1 00151] Synthesis of l-(2-amino-5-chlorophenyl)-1-phenyethan-1-ol.

To 2-amino-5- chlorobenzophenone (2.34 mmols, 541 mgs) in diethyl ether (lOmL ) under nitrogen atmosphere at 0 °C was added dropwise methylmagnesium iodide (3.12 mL, 3.0M in diethyl ether). The reaction mixture was stirred and left to warm to room temperature. After 5 hours, the mixture was cooled to 0 °C and ice chips were carefully added followed by cold water. Brine was added to separate the phases. The ether layer was separated. The aqueous layer was extracted with an equal amount of ether. The combined ether layers were dried over magnesium sulfate, filtered and concentrated under vacuum to yield the tertiary alcohol (2.14 mmols, 530 mgs). MS: (M+H) 248.

References:

WO2016/154039,2016,A1 Location in patent:Paragraph 00151