1. Product title:Sibutramine
2. Product parameter table:
|Appearance||Colorless or white crystalline powder||Main Effect||Lose weight|
|Brand Name||Kan Ying||Store-method||Cool Dry Place|
|Shelf Life||2 Years When
Sibutramine is indicated for obesity that cannot be reduced or controlled by exercise and dietary control, and can reduce and maintain weight loss. Treatment should be combined with a low-calorie diet and exercise. It is recommended that obese patients have a body mass index greater than or equal to 30kg/m or greater than or equal to 27kg/m with other risk factors (such as hypertension, diabetes, dyslipidemia, etc.).
The recommended starting dose is 50mg once daily, taken alone or with food in the morning. If weight loss is insufficient, the dose can be adjusted to 55mg per day after 4 weeks. If the patient cannot tolerate a dose of 50mg, it can be reduced to 5mg per day. The dose should be adjusted according to the patient's blood pressure and heart rate, and more than 65mg per day is not recommended.
1. Sibutramine in combination with other central appetite suppressants may cause severe hypertension and tachycardia. Sibutramine is therefore contraindicated with other central appetite suppressants.
1.5-HT reuptake inhibitors for the treatment of obesity.
2. Sibutramine, as a norepinephrine and 5-HT reuptake inhibitor, acts mainly through its metabolites. It can increase physiological satiety, reduce appetite, induce thermogenesis, increase energy consumption and reduce fat accumulation by inhibiting cell reuptake of monoamine information transfer factors such as 5-HT and norepinephrine. Obesity treatment for diet control, failure to lose weight through exercise and weight control
Sibutramine (106650-56-0) production method:
1, 3-dibromopropane was slowly dropped into the mixture of p-chlorophenonitrile, KOH and acetonitrile at 25℃. After dropping, continue stirring for 1h, add distilled water, and then extract with ethyl acetate. The extract was washed with water and saturated salt and dried. After filtration, decompression concentration and distillation, the fraction of 160℃/2.13kPa was collected to obtain compound (ⅰ) with yield of 73% ~ 74%.
Magnesium tablets were dissolved in anhydrous THF, and isobutyl bromine was dropped, and then reacted for 1h, and then anhydrous THF solution of compound (ⅰ) was added slowly, and then reflux for 4h, and cooled to room temperature. It was dropped into isopropyl alcohol solution of KBH4 and reflux for 4h. Cool, add water and extract with ethyl acetate. The extract was washed with water and saturated salt and dried. After filtration, the filtrate was decompressed and concentrated before distillation, and the fraction of 170℃/0.67kPa was collected to obtain compound (ⅱ) in 76% ~ 79% yield.
Compound (ⅱ), formic acid and 1/2 formaldehyde were stirred at 90 ~ 92℃ for 1h. Add another 1/2 formaldehyde solution, and continue to react for 1h. Cool to room temperature, stir and slowly pour into crushed ice of sodium hydroxide, then extract with ether. The extract was washed with saturated salt water and dried. After filtration, the filtrate was concentrated to obtain earthen yellow sibutramine with 94% yield. The analysis samples can be recrystallized with diethyl ether, melting point 52 ~ 53℃.
Sibutramine was dissolved in methanol, and concentrated hydrochloric acid was added to react at 50-60 'C for 10min. Decompression of methanol recovery to a small amount of crystallization precipitation, add water, stir, ice bath cooling. Sibutramine hydrochloride crude product was obtained by filtration and washing, and white crystalline Sibutramine hydrochloride was obtained by recrystallization with methanol-water, melting point 194℃, yield 83%.
5. Pictures of the product: