Synthesis method of 4'-halogenated methylbiphenyl-2-formic aid alkyl ester

• Main Authors: WANG ZHONGYU, ZHANG QUANQING
• Format: Patent
• Language: English
• Published: 17.02.2016
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a synthesis method of a 4'-halogenated methylbiphenyl-2-formic acid alkyl ester compound, and belongs to the technical field of organic synthesis. The method includes the following steps that 1, biphenyl-2-formic acid (I) and low alkyl alcohol are subjected to an esterification reaction under an acid catalyst to prepare biphenyl-2-formic acid alkyl ester (II); 2, the temperature in a four-mouth bottle containing biphenyl-2-formic acid alkyl ester (II), paraformaldehyde and a solvent is controlled to be within 20-50 DEG C, zinc halide is added, a dehydrating agent is added drop by drop, liquid chromatography monitoring is performed till the raw materials disappear about 2-5 h later, the reaction is finished, the temperature is lowered to the room temperature, an oil layer is washed, crystallization is performed to prepare 4'-halogenated methylbiphenyl-2-formic acid alkyl ester (III), and recrystallization purification is performed to prepare a pure product of 4'-halogenated methylbiphenyl-2-formic acid alkyl ester (III). According to the method, with biphenyl-2-formic acid as the starting raw material, the sartan drug intermediate 4'-halogenated methylbiphenyl-2-formic acid alkyl ester is prepared; the process is simple, conditions are easy to control, the raw materials are cheap and easy to get, production cost is low, environmental pollution is small, and the method is suitable for industrial production.