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[Studies on the synthesis of dl-ligustiphenol and its analogues]
1Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050.
Abstract:
S-( -- )-Ligustiphenol is a new sesquiterpene with anti-inflammatory and immunosuppressive activities. In order to study its pharmacological activities, the total synthesis of its racemat was carried out by a six-step reaction sequence including bromination of aldehyde, iodination of m - cresol, protection of phenolic hydroxyl, Grignard reaction, Aldol condensation, etc. The target compound was characterized by comparing its 1(H)-NMR, MS and IR spectra with natural ( -- )-ligustiphenol. In order to study the structure-activity relationships of ligustiphenol, it five analogues were designed and synthesized. The pharmacological screening of these analogues has been performed.