发明名称 Intermediates in the synthesis of indole analogs of mevalonolactone and derivatives thereof
摘要 Compounds of the formula <IMAGE> wherein one of R and Ro is <IMAGE> and the other is primary or secondary C1-6alkyl not containing an asymmetric carbon atom, C3-6cycloalkyl or phenyl(CH2)m-, wherein R4 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5a is hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, and m is 1, 2 or 3, with the provisos that both R5 and R5a must be hydrogen when R4 is hydrogen, R5a must be hydrogen when R5 is hydrogen, not more than one of R4 and R5 is trifluoromethyl, not more than one of R4 and R5 is phenoxy, and not more than one of R4 and R5 is benzyloxy, R2 is hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C3-6cycloalkyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R3 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, with the provisos that R3 must be hydrogen when R2 is hydrogen, not more than one of R2 and R3 is trifluoromethyl, not more than one of R2 and R3 is phenoxy, and not more than one of R2 and R3 is benzyloxy, X is -(CH2)n- or -CH=CH-, wherein n is 0, 1, 2 or 3, and Z is <IMAGE> wherein R6 is hydrogen or C1-3alkyl, and R7 is hydrogen, C1-3alkyl, 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.
申请公布号 US4739073(A) 申请公布日期 1988.04.19
申请号 US19850707854 申请日期 1985.03.04
申请人 SANDOZ PHARMACEUTICALS CORP. 发明人 KATHAWALA, FAIZULLA G.
分类号 C07D209/12;C07D209/18;C07D209/42;C07D405/06;C07F9/572;(IPC1-7):C07D405/06 主分类号 C07D209/12
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