ChemicalBook CAS DataBase List BUCLIZINE

BUCLIZINE synthesis

3synthesis methods

Product Name:BUCLIZINE
CAS Number:82-95-1
Molecular formula:C28H33ClN2
Molecular Weight:433.03

Buclizine is mainly used in the prevention of motion sickness and in combination with analgesics for treatment of migraine.

129-74-8
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$25.00/50mg

82-95-1
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$495.00/5 mg

Yield:-

Reaction Conditions:

with sodium hydroxide in ethanol;water; pH=5.8 at 25;

Steps:

2.2.4 Buclizine free-base (BCZ-FB)
To obtain BCZ-FB polycrystalline material, 1.0g of the raw material was solubilized at 25°C in 500mL of ethanol:water (1:1, v:v) mixture. After sonication for 10min, 1.0mol L^-1 NaOH solution was trickled into the vial until pH 5.8 was reached (optimized value to produce BCZ-FB absent of BCZHCl), which produced a significant amount of a white colloidal precipitate. The remaining procedures were the same as those applied to obtain the polycrystalline BCZH₂Cl₂ sample. The generation of BCZ-FB was confirmed by HPLC (chemical purity of 99.5% +/- 0.01), PXRD, IR, DSC, and TGA data (See Discussion). Unfortunately, several attempts using different crystal growth protocols to obtain BCZ-FB single crystals that were good enough for a single-crystal X-ray diffraction experiment were unsuccessful. Attempts to determine the crystal structure of BCZ-FB from powder X-ray diffraction data were also unsuccessful.

References:

Bitencourt, Monalisa;Doriguetto, Antonio Carlos;Freitas, Jennifer Tavares Jacon;Viana, Andre Luiz Machado;Viana, Olimpia Maria Martins Santos;de Melo, Cristiane Cabral [International Journal of Pharmaceutics,2020,vol. 589]

877-65-6 Synthesis