
Journal of the Serbian Chemical Society p. 1205 - 1212 (2015)
Update date:2022-08-03
Topics:
Li, Yu-Wen
Ma, Cui-Li
Highly practical, four-step synthesis of gastrodin was developed using penta- O-acetyl-β-D-glucopyranose and p-cresol as glycosyl donor and glycosyl acceptor, respectively, in 58.1% overall yield. As the initial step, the penta-O-acetyl-β-D-glucopyranose was treated with p-cresol in the presence of BF3 ?Et2O as catalyst to generate 4-methylphenyl 2,3,4,6-tetra-O-acetyl-β-D- -glucopyranoside in 76.3% yield. Further, this product was subjected to radical bromination with N-bromosuccinimide (NBS) to provide 4-(bromomethyl)phenyl 2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside in 91% yield. Subsequently, reaction of 4-(bromomethyl)phenyl 2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside with a solution of acetone and saturated aqueous sodium bicarbonate led to 4-(hydroxymethyl)phenyl 2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside in 93% yield. Finally, global deprotection of 4-(hydroxymethyl)phenyl 2,3,4,6-tetra-O- -acetyl-β- D-glucopyranoside under Zemplen conditions furnished gastrodin in 90% yield. Compared to the previously reported methods, this protocol has the advantages of operational simplicity, chromatography-free separation, high overall yield, inexpensive and common reagents as well as less waste pollutants, rendering it an alternative suitable for industrial production.
View MoreContact:+49-4101-3053-0
Address:Waldhofstrasse 14 ,25474 Ellerbek Germany
NEW FORTUNE INDUSTRIAL CO.,LTD.
website:http://newfortune.lookchem.com/
Contact:+86-25-8645-9456
Address:C4-105 GREEN ISLAND FLOWER TOWN
Guangzhou Puho Pharmaceutical Technology Co. Ltd.
Contact:86-20-29848035/29848075
Address:No.166, Chaoyang East Road, Panyu District, Guangzhou City, Guangdong Province
JiangXi Hong Run Chemical Co., Ltd
Contact:+86-0791-88521351
Address:XingHuo industrial zone in YongXiu county
Shenzhen Sunrising Industry Co., ltd.
Contact:+86 755 86571158 / 86571159 / 86571160
Address:2108 ZHENYE INT. BUSINESS CENTER,NO.3101-90 QIANHAI RD, NANSHAN,SHENZHEN, CHINA
Doi:10.1139/cjc-2017-0745
(2019)Doi:10.1021/jo00336a004
(1981)Doi:10.1002/ejoc.200400676
(2005)Doi:10.1080/00304948.2015.1005986
(2015)Doi:10.1021/jm00143a014
(1981)Doi:10.1002/jhet.3914
(2020)