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ChemicalBook CAS DataBase List CINACALCET
226256-56-0

CINACALCET synthesis

5synthesis methods
Benzeneacetic acid, α-hydroxy-, (αR)-, compd. with (αR)-α-methyl-1-naphthalenemethanamine (1:1)

1073144-62-3
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CINACALCET

226256-56-0
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Yield:226256-56-0 100%

Reaction Conditions:

with potassium carbonate in water at 60 - 65; for 20 h;

Steps:

6

Example 6; Preparation of cinacalcet base - from a salt of (R)-i-naphthylethylamine; Purified water (400 ml) was taken in a reaction vessel. Potassium carbonate (0.77 moles, 107 gms) and the product of Example 3 (0.39 moles, 110 gms) were added under stirring. The reaction mixture was heated to 60-650C. The compound obtained from example 4 (0.26 moles, 83 gms) was added maintaining the temperature of the reaction mass at 60- 650C for 20 hours under stirring. After cooling the mass to a temperature of 20-250C, ethyl acetate (850 ml) was added and stirred. The separated organic layer was washed with purified water (2 x 400 ml) and then washed with saturated brine solution (2 x 400 ml).The solvent was removed from the organic layer by distillation under vacuum to obtain cinacalcet base (91 gms, yield 100%).

References:

WO2010/100429,2010,A1 Location in patent:Page/Page column 20-21

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