METHOD FOR SYNTHESIZING D-PARA-HYDROXYPHENYLGLYCINE METHYL ESTER

WIPO Patent Application WO/2016/202252

A1

The present invention relates to the field of compound synthesis and discloses a method for synthesizing D-para-hydroxyphenylglycine methyl ester. The method comprises the steps of: (1) in the presence of thionyl chloride, carrying out an esterification reaction of D-para-hydroxyphenylglycine resolving agent salt and methanol to obtain a D-para-hydroxyphenylglycine methyl ester resolving agent salt; (2) dropwise adding the D-para-hydroxyphenylglycine methyl ester resolving agent salt and an alkaline metal hydroxide to an aqueous D-para-hydroxyphenylglycine methyl ester solution at 10-15°C, controlling the pH value of the system at 6.5-7 during the dropwise addition, after completing the dropwise addition of the D-para-hydroxyphenylglycine methyl ester resolving agent salt, continuing the dropwise addition of the alkaline metal hydroxide until the pH value of the system is 7.5-8, then growing crystals under the conditions of a temperature of 10-15°C and the pH value of 7.5-8, and subsequently filtering the resultant crystallization liquid to obtain D-para-hydroxyphenylglycine methyl ester crystals and a mother liquor. With the adoption of the method provided by the present invention, D-para-hydroxyphenylglycine methyl ester can be produced with a higher yield.

WANG QIBIN (CN)

PCT/CN2016/085804

December 22, 2016

June 15, 2016

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SHANXI XINBAOYUAN PHARMACEUTICAL CO LTD (CN)

C07C229/36; C07C227/18; C07C227/42

CN104892444A	2015-09-09
CN103113250A	2013-05-22
CN103553949A	2014-02-05
CN104529801A	2015-04-22

RUNPING&PARTNERS (CN)
北京润平知识产权代理有限公司 (CN)

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