📜Triphenyl(Phenylethynyl)Phosphonium Bromide置于氢溴酸体系中,用 乙醇,乙腈 作为反应溶剂,化学反应 19.0H,反应生成 (苯甲酰基甲基)三苯基溴化膦 参考文献:Reaction Of Triphenyl(Phenylethynyl)Phosphonium Bromide With α-Aminoethers,Dipiperidinomethane,And Secondary Amines 标题:Reaction Of Triphenyl(Phenylethynyl)Phosphonium Bromide With α-Aminoethers,Dipiperidinomethane,And Secondary Amines 摘要:The Reactions Of Triphenyl(Phenylethynyl)Phosphonium Bromide With (Alpha-Aminoethers Lead To Formation Of Triphenyl(2-Amino-2-Phenylvinyl)Phosphonium Bromides. In The Case Of Acyclic Aminoethers,This Reaction Is Accompanied By The Formation Of The Corresponding Amine Hydrobromide And Triphenylphosphine Oxide By A Scheme Analogous To That Of Alkaline Hydrolysis Of Phosphonium Salts And Involving Attack Of The Amine On The Phosphorus Atom. The Reaction Of The Same Salt With Diethyl-Or Dipropylamine Affords Hydrobromides Of The Latter,While With Piperidine,Together With Salts,Its Adduct By The Triple Bond Is Formed. Piperidinomethane With The Same Salt Forms Triphenylphosphonium (2-Phenyl-2-Piperidinovinyl)Phosphonium Bromide. DOI:10.1134/s1070363207050088
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.