Intermediates in the synthesis of indole analogs of mevalonolactone and derivatives thereof
申请(专利)号:
06/707854
申请日期:
03/04/1985
公开/公告号:
US4739073
公开/公告日期:
04/19/1988
申请(专利权)人:
Sandoz Pharmaceuticals Corp. (E. Hanover, NJ)
被引量:
摘要:
Compounds of the formula ##STR1## wherein one of R and R o is ##STR2## and the other is primary or secondary C 1 -6 alkyl not containing an asymmetric carbon atom, C 3 -6 cycloalkyl or phenyl(CH 2 ) m --, wherein R 4 is hydrogen, C 1 -3 alkyl, n-butyl, i-butyl, t-butyl, C 1 -3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R 5 is hydrogen, C 1 -3 alkyl, C 1 -3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R 5a is hydrogen, C 1 -2 alkyl, C 1 -2 alkoxy, fluoro or chloro, and m is 1, 2 or 3, with the provisos that both R 5 and R 5a must be hydrogen when R 4 is hydrogen, R 5a must be hydrogen when R 5 is hydrogen, not more than one of R 4 and R 5 is trifluoromethyl, not more than one of R 4 and R 5 is phenoxy, and not more than one of R 4 and R 5 is benzyloxy, R 2 is hydrogen, C 1 -3 alkyl, n-butyl, i-butyl, t-butyl, C 3 -6 cycloalkyl, C 1 -3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R 3 is hydrogen, C 1 -3 alkyl, C 1 -3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, with the provisos that R 3 must be hydrogen when R 2 is hydrogen, not more than one of R 2 and R 3 is trifluoromethyl, not more than one of R 2 and R 3 is phenoxy, and not more than one of R 2 and R 3 is benzyloxy, X is --(CH 2 ) n -- or --CHCH--, wherein n is 0, 1, 2 or 3, and Z is ##STR3## wherein R 6 is hydrogen or C 1 -3 alkyl, and R 7 is hydrogen, C 1 -3 alkyl, n-butyl, i-butyl, t-butyl, benzyl or M, wherein M is a pharmaceutically acceptable cation, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level, and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
展开
通过文献互助平台发起求助,成功后即可免费获取论文全文。
相似文献
参考文献
引证文献
引用走势
辅助模式
引用
文献可以批量引用啦~
欢迎点我试用!