Tesofensine Chemical Properties

storage temp. 

Hygroscopic, -20°C Freezer, Under inert atmosphere

solubility 

Chloroform (Slightly), Methanol (Slightly)

form 

Solid

color 

Off-White to Light Yellow

InChI

InChI=1/C17H23Cl2NO/c1-3-21-10-14-13(9-12-5-7-17(14)20(12)2)11-4-6-15(18)16(19)8-11/h4,6,8,12-14,17H,3,5,7,9-10H2,1-2H3/t12?,13-,14-,17?/s3

InChIKey

VCVWXKKWDOJNIT-KJBRQMMRNA-N

SMILES

C12N(C)C(CC1)C[C@H](C1=CC=C(Cl)C(Cl)=C1)[C@H]2COCC |&1:7,16,r|

Tesofensine Usage And Synthesis

Uses

Tesofensine, is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is currently in clinical development for the treatment of obesity.

benefits

One of the most significant benefits of Tesofensine is that it can help patients achieve long-term weight loss goals. Unlike other medications, this drug has been shown to produce results when taken within 6 months. Another benefit of Tesofensine is its ability to improve metabolic function in overweight individuals. This medication helps regulate blood sugar levels and reduce insulin resistance by suppressing appetite and reducing fat absorption. When the body is insulin resistant, it creates a condition called diabetes.

Side effects

Common side effects include dry mouth, headache, nausea, insomnia, diarrhea, and constipation. Blood pressure and heart rate were increased by 1–3 mmHg and up to 8 bpm, respectively.

Synthesis

The main synthetic method of Tesofensine is as follows: first methyl esterify with tropinone, then reduce to alcohol intermediate by reducing agent, then make alkene intermediate by dehydrating agent, then alkene make intermediate ester compound by format reaction, then reduce ester to alcohol intermediate by red aluminum, and finally etherify to get the final product crude product by alcohol intermediate, and finally purify the obtained product by column chromatography. The above route, the reaction steps are long, high-risk reaction steps, harsh reaction conditions, which also use rare and noble reagents, the overall yield is low, the synthesis cost is quite high, so that can not achieve industrial production.

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