NEBIVOLOL HCL synthesis
- Product Name:NEBIVOLOL HCL
- CAS Number:169293-50-9
- Molecular formula:C22H26ClF2NO4
- Molecular Weight:441.9
929706-85-4
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$85.00/1mg
169293-50-9
74 suppliers
$240.00/50mg
Yield: 95%
Reaction Conditions:
Stage #1:N-benzylnebivolol with 20% palladium hydroxide-activated charcoal;hydrogen;acetic acid in water for 12 h;Large scale;
Stage #2: with sodium chloride in water for 8 h;Large scale;
Steps:
9 Synthesis of Nebivolol hydrochloride
20 % Pd(OH)2/C (50 % wet) (approximately 24 g) is added to a suspension of (RSSS)/(SRRR)-Nbenzylnebivolol VIc (1.5 Kg) in AcOH (10 Kg) and H2O (1 Kg) . The suspension is left under stirring in an H2 atmosphere for approximately 12 hours. At the end of the reaction, the catalyst is filtered off and an aqueous solution of NaC1 (1.06 Kg of NaC1 in 21 kg of H20) is added under stirring, with observation of the spontaneous precipitation of a white solid. After stirring for at least 8 hours, the suspension is filtered and the solid is washed with 400 mL of H2O (6 Kg), then with EtQH (3 Kg), so as to obtain the nebivolol hydrochloride as a white solid (1.1 Kg, yield 95 %, purity HPLC 99.7 %)
References:
MENARINI INTERNATIONAL OPERATIONS LUXEMBOURG S.A.;BARTOLI, Sandra;MANNUCCI, Serena;GRISELLI, Alessio;STEFANINI, Alessio WO2017/125900, 2017, A1 Location in patent:Page/Page column 38-39
929706-85-4
20 suppliers
$85.00/1mg
929706-85-4
20 suppliers
$85.00/1mg
169293-50-9
74 suppliers
$240.00/50mg