Synthesizing method of weight loss drug orlistat intermediate
A technology of orlistat and a synthetic method, which is applied in the field of synthesis of key intermediates of weight-loss drugs, can solve problems such as long routes and expensive synthesis costs, and achieve the effects of simple operation process, simple operation, and reduced production costs
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[0018]1. Synthesis of compound (3): Dissolve Evans (Evans) chiral auxiliary (5.0g, 19.9mmol, 1.0eq) in dichloromethane (60mL) at -78°C and under the protection of nitrogen , slowly added titanium tetrachloride (4.37mL, 39.8mmol, 1.8eq) dropwise to the mixed solution, the solution turned yellow after the addition, and after stirring for 5 minutes, slowly added N, N -Diisopropylethylamine (6.93mL, 2.09mmol, 1.8eq), once added to the reaction system, the solution quickly turns dark red, after the dropwise addition at -78°C, continue to stir at this temperature for 1 hour, Then, the raw material n-dodecaldehyde (2) (4.40g, 23.88mmol, 1.2eq) was dissolved in dichloromethane (20mL), and then this solution was slowly injected into the above reaction system, reacted for 2 hours, and detected by TLC After finding that Evans (Evans) chiral auxiliary agent has reacted, add saturated ammonium chloride solution (20mL) to the mixing system and quench the reaction system, then extract with d...
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