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ChemicalBook CAS DataBase List 4,4-DIFLUORO-N-((1S)-3-HYDROXY-1-PHENYLPROPYL)CYCLOHEXANE-1-CARBOXAMIDE
376348-77-5

4,4-DIFLUORO-N-((1S)-3-HYDROXY-1-PHENYLPROPYL)CYCLOHEXANE-1-CARBOXAMIDE synthesis

4synthesis methods
-

Yield:-

Reaction Conditions:

with N-ethyl-N,N-diisopropylamine;HATU in N,N-dimethyl-formamide at 18 - 25; for 144 h;

Steps:

G.1

Method G; Preparation of 4,4-difluoro-A^-[(15)-3-oxo-1 -phenylpropyljcyclohexanecarboxamide; Step 1: Preparation of 4,4-difluoro-Af-[(l'S)-3-hydroxy-l-phenylpropyl]cyclohexanecarboxamide; To a mixture of 4,4'-difluorocyclohexylcarboxylic acid (2.83g) and HATU (6.56g) indimethyl formamide (15ml) was added (S)-3-amino-3-phenylpropanol (2.37g) anddiisopropyl ethylamine (6.83ml). The mixture was allowed to stir at room temperature for 6days. The reaction mixture was poured into water (600ml) and extracted with ethyl acetate(2x200ml). The organics were washed with IN NaOH (200ml), brine (200ml), dried (MgSO4)and concentrated. The residue was purified by silica chromatography eluting with diethylether / iso-hexane to give the sub-title compound as a white solid. Yield 2.81g. NMR (d6DMSO): 1.66 (bm, 8H), 2.0 (m, 2H), 2.3 (m, 1H), 3.3 (m, 2H), 4.45 (t, 1H), 4.9 (m, 1H), 7.2(m, 5H), 8.2 (m, 1H).

References:

WO2006/1752,2006,A1 Location in patent:Page/Page column 70

376348-78-6 Synthesis
4,4-DIFLUORO-N-((1S)-3-OXO-1-PHENYLPROPYL)CYCLOHEXANE-1-CARBOXAMIDE

376348-78-6
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4,4-DIFLUORO-N-((1S)-3-HYDROXY-1-PHENYLPROPYL)CYCLOHEXANE-1-CARBOXAMIDE

376348-77-5
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