专利号:US-4739073-A 优先权日:1983-11-04 标题:Intermediates in the synthesis of indole analogs of mevalonolactone and derivatives thereof 发明人:KATHAWALA FAIZULLA G 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula wherein one of R and Ro is 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 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.
专利号:US-5354772-A 优先权日:1982-11-22 标 题:Indole analogs of mevalonolactone and derivatives thereof 发明人:KATHAWALA FAIZULLA G 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula wherein one of R and Ro is 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 wherein R6 is hydrogen or C1-3alkyl, and R7 is hydrogen, R7b or M, wherein R7b is a physiologically acceptable and hydrolyzable ester group, and 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 hyperliopoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
专利号:CA-3012054-C 优先权日:2016-03-16 标 题 :Microbial synthesis of isoprenoid precursors, isoprenoids and derivatives including prenylated aromatics compounds
参考标题:An Efficient, Second-Generation Synthesis Of The Signature Dioxabicyclo[3.2.1]Octane Core Of (+)-Sorangicin A And Elaboration Of The (Z,Z,E)-Triene Acid System 作者:Amos B. Smith,,Shuzhi Dong |发布日期:2009.3.5 摘要:An Efficient, Second-Generation Synthesis Of The Signature Dioxabicyclo[3.2.1]Octane Core Of (+)-Sorangicin A (1), In Conjunction With An Effective, Stereocontrolled Protocol To Arrive At The Requisite (Z,Z,E)-Triene Acid System Has Been Developed. Highlights Of The Core Construction Entail A Three-Component Union, A Khmds-Promoted Epoxide Ring Formation−ring Opening Cascade, A Takai Olefination, And
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参考文献:10.1016/j.ejmech.2014.11.020 摘要:Cai H, Liu Q, Gao D, Wang T, Chen T, Yan G, Chen K, Xu Y, Wang H, Li Y, Zhu W. Novel fatty acid binding protein 4 (FABP4) inhibitors: Virtual screening, synthesis and crystal structure determination. European Journal of Medicinal Chemistry. 2015 Jan;90():241–50. doi: 10.1016/j.ejmech.2014.11.020.