
Helvetica Chimica Acta p. 1159 - 1168 (1996)
Update date:2022-08-04
Topics:
Buerli, Roland
Vasella, Andrea
The synthesis of monomers of type C (Scheme 1) is described.In a first approach, chloro-acetyl-addition to the dioxolane 2 (Scheme 2), followed by treatment of the resulting chlorides 3 (α-D/β-D 1:3) with excess AgOTf and Bu3SnCCSiMe3 gave the axial C-alkynyl-glycoside 4 (31percent) and the C-arylglycoside 5 (29percent).The structure of the dialkyne 6, obtained by deacetylation of 4, was established by X-ray analysis.The yield of the C-alkynylglycoside was slightly improved by protecting the C(4)-ethynyl group as the triethylsilyl derivative, but not by substituing the benzyl by allyl or 2,6-difluorobenzyl groups.Silylation of the diol 1 with (chloro)diethyl<2-(trimethylsilyl)ethynyl>silane (19) resulted in 90percent of the monosilyl ether 20.HO-C(3) of 20 should favor coordination of a Lewis acid to O-C(6), and intramolecular, inverting acetal opening should lead to the product of axial alkynylation.Indeed, treatment of 20 with in situ generated BuAlCl2, followed by treatment of the crude product with 0.1 M HCl in MeOH, gave the dialkynylated triol 22 in yields of 85 to 90percent.Under similar conditions, the disilyl ether 21 reacted more slowly to 22 (75percent).The slower reaction correlates with the assumed intramolecular interaction of the precoordinated Lewis with O-C(6) in 20.
View MoreLianYunGang Chiral Chemical(CHINA) CO.,LTD
Contact:+86-518-83616958 +86-519-82884848
Address:LianYunGang Chemical Industry Park (JiangSu)
Wuhan Kemi-Works Chemical Co., Ltd
website:http://www.kemiworks.com
Contact:86-27-85736489
Address:Rm. 1503, No. 164, Jianghan North Rd., Wuhan, 430022 China
Liaoyang hengye Chemical Co., Ltd.
Contact:86-419-5850866
Address:North Old Xiaoxiao Road,Yantai District, Dengta, Liaoyang, Liaoning, China
Shanghai Goyic Pharmaceutical&Chemical Co,. Ltd
Contact:+86-021-60275964
Address:No. 528 ruiqing road
Anhui Xinyuan Technology Co.,Ltd
Contact:0086-559-3515800
Address:No.16 Zijin Rd, Circular Economic Zone, Huizhou District, Huangshan Anhui China
Doi:10.1002/cber.19961290804
(1996)Doi:10.1016/0960-894X(96)00315-0
(1996)Doi:10.1016/0960-894X(96)00307-1
(1996)Doi:10.1246/bcsj.71.1193
(1998)Doi:10.1016/0022-1139(93)02901-P
(1994)Doi:10.1016/0957-4166(96)00225-X
(1996)