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ChemicalBook CAS DataBase List PHENTERMINE
122-09-8

PHENTERMINE synthesis

12synthesis methods
Phentermine is prepared by converting the condensation product of benzaldehyde and nitropropane to the corresponding aminoalcohol followed by transformation to the chloroamine and then catalytic hydrogenation .
Synthesis_122-09-8
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Yield:122-09-8 41%

Reaction Conditions:

with phosphorus;hydrogen iodide in water at 135;

Steps:

1 Synthesis of 1e
P (677 mg, 22 mmol) was slowly added to the solution of ld (1.5 g, 9.1 mmol) in HI (22 mE 45% in water) at room temperature. The mixture was stirred at 135° C. overnight, and then cooled to room temperature. Water (100 mE) was added to the above mixture, which was filtered. Saturated aqueous Na25203 solution (100 mE) was added to the filtrate and was made basic with 40% NaOH (20 mE). The resulting mixture was extracted with ethyl acetate (100 mEx3). The combined ethyl acetate layer was washed with water and dried over anhydrous Na2504 and evaporated. The residue was purified by silica column chromatography (DCM: MeOH30:1, v:v) to provide R’ (0.55 g, 41% yield).

References:

HELSINN HEALTHCARE SA;Giuliano, Claudio;Daina, Antoine;Pietra, Claudio US2017/275301, 2017, A1 Location in patent:Paragraph 0198; 0201

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