专利号:US-4973704-A 优先权日:1985-10-25 标题 :Pyrrolyl intermediates in the synthesis of pyrrole analogs of mevalonolactone and derivatives thereof 发明人：WAREING JAMES R 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula wherein R1 is C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R5, R6 and R7 are as defined below, R2 is C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R8, R9 and R10 are as defined below, R3 is hydrogen, C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R11, R12 and R13 are as defined below, R4 is hydrogen, C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R14, R15 and R16 are as defined below, X is -(CH2)m-, -CH=CH-, -CH=CH-CH2-or -CH2-CH=CH-, wherein m is 0, 1, 2 or 3, and Z is wherein R17 is hydrogen or C1-3alkyl, and R18 is hydrogen, R19 or M, wherein R19 is a physiologically acceptable ester group, and M is a pharmaceutically acceptable cation, wherein each of R5, R8, R11 and R14 is independently hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, bromo, phenyl, phenoxy or benzyloxy, each of R6, R9, R12 and R15 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, bromo, phenoxy or benzyloxy, and each of R7, R10, R13 and R16 is independently hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, with the provisos that not more than one substituent on each of Rings A, B, C and D independently is trifluoromethyl, not more than one substituent on each of Rings A, B, C and D independently is phenoxy, and not more than one substituent on each of Rings A, B, C and D independently is benzyloxy, with the provisos that (i) the -X-Z group is in the 2- or 3-position of the pyrrole ring, (ii) the -X-Z group is ortho to both R1 and R2 and (iii) R3 is ortho to R2, 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-4851427-A 优先权日:1985-10-25 标 题 :Pyrrole analogs of mevalonolactone, derivatives thereof and pharmaceutical use 发明人：WAREING JAMES R 权利人:SANDOZ PHARMACEUTICALS CORP 摘要:Compounds of the formula wherein R1 is C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R5, R6 and R7 are as defined below, R2 is C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R8, R9 and R10 are as defined below. R3 is hydrogen, C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or wherein R11, R12 and R13 are as defined below, R4 is hydrogen, C1-6alkyl not containing an asymmetric carbon atom, C7-7cycloalkyl or wherein R14, R15 and R16 are as defined below, X is -(CH2)m-, -CH=CH-, -CH=CH-CH2- or -CH2-CH=CH-, wherein m is 0, 1, 2 or 3, and Z is wherein R17 is hydrogen or C1-3alkyl, and R18 is hydrogen, R19 or M, wherein R19 is a physiologically acceptable ester group, and M is a pharmaceutically acceptable cation, wherein each of R5, R8, R11 and R14 is independently hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, bromo, phenyl, phenoxy or benzyloxy, each of R6, R9, R12 and R15 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, bromo, phenoxy or benzyloxy, and each of R7, R10, R13 and R16 is independently hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, with the provisos that not more than one substituent on each of Rings A, B, C and D independently is trifluoromethyl, not more than one substituent on each of Rings A, B, C and D independently is phenoxy, and not more than one substituent on each of Rings A, B, C and D independently is benzyloxy, with the provisos that (i) the -X-Z group is in the 2- or 3-position of the pyrrole ring, (ii) the -X-Z group is ortho to both R1 and R2, and (iii) R3 is ortho to R2, 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.
参考标题:Synthesis Of Unsymmetrical Tetrathiafulvalene Derivatives Via Me3Al-Promoted Reactions Of Organotin Compounds With Esters 作者:Jun-Ichi Yamada,Shyûji Satoki,Sachinori Mishima,Nobutaka Akashi,Kouhei Takahashi,Nobuyuki Masuda,Yasushi Nishimoto,Satoshi Takasaki,Hiroyuki Anzai |发布日期:1996.1.1 摘要:In Addition, The Synthesis Of Diselenadithiafulvalene Derivatives (25-28) Could Be Accomplished By Me(3)Al-Mediated Reaction Of Tin Thiolate (2A) Or Selenolates (3D And 5) With Esters (22A, 22D, And 24). Furthermore, The Application Of The Me(3)Al-Promoted Reaction Of Tin Thiolate (34) With Esters (11A-B, 22A-D, And 35A-B) For The Synthesis Of Unsymmetrical Ttfs-Fused Donors Enabled Us To Obtain Various
合成参考文献
摘要:Kawęcki, R., Science of Synthesis Knowledge Updates, (2011) 3, 204. 摘要:Leung, M.-k.; Chou, C.-M.; Luh, T.-Y., Science of Synthesis Knowledge Updates, (2018) 2, 449.
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