Journal of Medicinal Chemistry p. 786 - 790 (1983)
Update date:2022-08-05
Topics:
Collins
Dajani
Pappo
Gasiecki
Bianchi
Woods
The synthesis and gastric antisecretory activities of the Δ4,5-cis, Δ4,5-trans, and 4,5-acetylenic analogues of 15-deoxy-16-hydroxy-16-methyl prostaglandin E1 methyl ester are described. The key step in the preparation of these compounds involved the stereospecific conjugate addition of a cuprate reagent to the appropriate cyclopentenones. Although the trans and acetylenic derivatives were weak inhibitors of gastric acid secretion, the cis olefin was more potent and longer acting than the saturated parent compound. Selectivity with respect to unwanted diarrheagenic effects was found to be improved over that of both the parent 16-hydroxy compound and the reference standards, (15S)-15-methyl- and 16,16-dimethylprostaglandin E2.
View MoreShanghai Rainbow Chemistry Co., Ltd.
Contact:+86-21-64968086-5815/5812
Address:3rd floor, Building 7, 251 Faladi Road, Zhangjiang Hi-Tech Park, Pudong District, Shanghai, P.R. China
Beijing Mesochem Technology Co.,LTD
website:http://www.mesochem.com
Contact:0086-10-57862036
Address:2301, Floor 23, Building 9 Lippo Plaza, Yard 8 Ronghua Middle Road, ETDZ, Beijing, China
Shenzhen HwaGen Pharmaceutical Co., Ltd
website:http://www.rafflespt.com
Contact:+86-752-5538396
Address:Guangdong Huizhou China
Refine Chemicals Science & Technology Technology Developing Co., Ltd.
Contact:+86-22-87899130
Address:No.12,west keyan road,Tianjin City
Lianyungang Ningkang Chemical Co., Ltd
Contact:.+86-518-88588008
Address:http://www.chemnk.com
Doi:10.1002/anie.201602219
(2016)Doi:10.1021/jo00334a057
(1981)Doi:10.1007/BF02236433
(2000)Doi:10.1021/ja00310a037
(1985)Doi:10.1039/b407067d
(2004)Doi:10.1021/ja052487n
(2005)