CAS: 93957-49-4; 3-(4-Fluorophenyl)-1-Isopropyl-1H-Indole

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CAS号93957-51-8 1-(4-氟苯基)-2-(异丙... | CAS号101125-32-0 3-(4-氟苯基)吲哚 | CAS号75-26-3 2-溴丙烷 | CAS号16885-99-7 (9ci)-1-(1-甲基乙基... | CAS号1038997-83-9 (4-fluorophenyl... | CAS号768-52-5 N-异丙基苯胺 | CAS号456-04-2 2-氯-4'-氟苯乙酮 | CAS号120-72-9 吲哚 | CAS号93957-50-7 (E)-3-[3'-(4"-氟... | CAS号100-61-8 N-甲基苯胺 | CAS号129332-30-5 费耐力 | CAS号101125-34-2 3-(4-氟苯基)-1-异丙基...

N-异丙基苯胺置于盐酸,Zinc(II) Chloride体系中,用 乙醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 3-(4-氟苯基)-1-异丙基-1H-吲哚
参考文献:含有氟伐他汀核的吲哚衍生物的 合成,晶体研究和体内降血脂活性†
标题:含有氟伐他汀核的吲哚衍生物的 合成,晶体研究和体内降血脂活性†
摘要:为制备更好的氟伐他汀类似物来治疗高脂血症的努力的一部分,我们已经通过甲醇介导的claisen-Schmidt醛醇缩合反应合成了一些含有氟伐他汀核的吲哚衍生物.通过ft-Ir,1 H NMR,13 C NMR和lcms光谱分析对新合成的分子进行表征.通过x射线衍射研究阐明了5B,5C,5G和5H的结构参数.研发了所有化合物的体内抗高血脂活性和组织病理学研究.在5A-l中,化合物5C和5I除血清高密度脂蛋白水平升高外,血清总胆固醇,甘油三酸酯,低密度脂蛋白和极低密度脂蛋白显着降低.与标准氟伐他汀药物相比,化合物5C和5I表现出明显的细胞质脂肪浸润以及颗粒变性.可以想象,药物类似物的合成可以产生更有效的治疗效果.另外,研发了最有效的降血脂药5C与人血清白蛋白hsa之间的相互作用.化合物5C可以主要通过以下方式与hsa可逆结合 一种涉及形成络合物的机理,其中氢键和疏水相互作用都是主要作用力.
DOI:10.1039/c5Ra02908B

专利信息

专利号:US-5118853-A
优先权日:1988-10-13
标题:Processes for the synthesis of 3-disubstituted aminoacroleins
发明人：LEE GEORGE T; REPIC OLJAN
权利人:SANDOZ LTD
摘要:Process for the synthesis of compounds of the formula ##STR1## comprising the steps of (i) reacting a compound of the formula ##STR2## with oxalyl chloride or oxalyl bromide to form the corresponding compound of the formula ##STR3## (ii) reacting said compound of the formula ##STR4## with a compound of the formula ##STR5## to form the corresponding compound of the formula ##STR6## (iii) hydrolyzing said compound of the formula ##STR7## to obtain the corresponding compound of the formula ##STR8## the use of the compounds of the formula ##STR9## for the synthesis of the compounds of the formula ##STR10## and the use of the intermediates of Formula VII for the direct synthesis of the compounds of Formula II, n wherein n R 1 is C 1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 1b is phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 2 is C 1-3 alkyl, n one of R 3 and R 4 is ##STR11## 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 -, n wherein n R 7 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, n R 8 is hydrogen, C 1-3 alkyl, C 1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, n R 9 is hydrogen, C 1-2 alkyl, C 1-2 alkoxy, fluoro or chloro, and n m is 1, 2 or 3, with the provisos that not more than one of R 7 and R 8 is trifluoromethyl, not more than one of R 7 and R 8 is phenoxy, and not more than one of R 7 and R 8 is benzyloxy, n R 5 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, and n R 6 is hydrogen, C 1-3 alkyl, C 1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy, or benzyloxy, with the provisos that not more than one of R 5 and R 6 is trifluoromethyl, not more than one of R 5 and R 6 is phenoxy, and not more than one of R 5 and R 6 is benzyloxy, n R 10 is C 1-6 alkyl, each X is chloro or bromo, and each X.sup.⊖ is chloride or bromide.

专利号:US-5290946-A
优先权日:1988-10-13
标 题 :Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes
发明人：LEE GEORGE T; KAPA PRASAD K; REPIC OLJAN
权利人:SANDOZ LTD
摘要:A process for synthesizing compounds of the formula ##STR1## utilizing, as intermediates, oxalyl chloride or bromide and compounds of the formulae R 1 R 2 N--CHO and CH 2 â•?CH--O--R 10 are processes for synthesizing compounds of the formula ##STR2## utilizing, as intermediates, compounds of Formula I wherein R 1 is phenyl or substituted phenyl or intermediates in the synthesis of the compounds of formula I which intermediates have the formula ##STR3## wherein R 1 is C 1-3 alkyl, phenyl or phenyl substituted by 1 to 3 substituents each of which is independently C 1-3 alkyl, C 1-3 alkoxy, fluoro, chloro, bromo or nitro (maximum of two nitro groups), n R 2 is C 1-3 alkyl, n R 10 is C 1-6 alkyl, n X.sup.⊖ is chloride or bromide, and n R 3 -R 6 are as defined in the specification. n The compounds of Formula II are intermediates in the synthesis of known HMB-CoA reductase inhibitors which inhibit the biosynthesis of cholesterol and are useful as antihyperchloesterolemic gents.

专利号:US-9085538-B2
优先权日:2010-07-26
标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof
发明人：CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO
权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS
摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.

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:US-7091382-B2
优先权日:2003-05-13
标题 :Synthesis of N-methyl-N-phenylaminoacrolein
发明人：BANFI ALDO; MANCINI ALFREDO
权利人:CLARIANT LSM ITALIA SPA
摘要:A process is disclosed for manufacturing N-methyl-N-phenylaminoacrolein of formula (I) n nwhich comprises reacting N-methylformanilide and an alkyl vinyl ether of formula (III)n n nwherein R is a C 3 –C 4 alkyl, said process being characterized in that the reaction between N-methylformanilide and said alkyl vinyl ether of formula (III) is carried out in the presence of phosgene, diphosgene or triphosgene in a solvent selected from dioxane, acetonitrile and/or chlorobenzene.