CAS: 1006-94-6; 5-Methoxyindole

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99275-47-5 10501-17-4 396091-50-2

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4-硝基间甲苯酚置于palladium On Activated Charcoal 氢气,Sodium Methylate体系中,用 N,N-二甲基甲酰胺,苯 用作溶剂,25.0 °C,303.98 Kpa 条件下,反应 49.25H,反应生成5-甲氧基吲哚
参考文献:A Versatile And Efficient Construction Of The 6H-Pyrido[4,3-B]Carbazole Ring System. Syntheses Of The Antitumor Alkaloids Ellipticine,9-Methoxyellipticine,And Olivacine,And Their Analogs
标题:A Versatile And Efficient Construction Of The 6H-Pyrido[4,3-B]Carbazole Ring System. Syntheses Of The Antitumor Alkaloids Ellipticine,9-Methoxyellipticine,And Olivacine,And Their Analogs
摘要:A General And Efficient Synthesis Of The 6H-Pyrido[4,3-B]Carbazole Ring System Is Described,In Which The Key Steps Are (1) Regioselective Acylation Of A 2-Lithio-1-(Phenylsulfonyl)Indole (14) With 3,4-Pyridinedicarboxylic Acid Anhydride (10),(2) Cyclization Of The Deprotected Keto Acid 17 To Keto Lactam 19 With Acetic Anhydride,And (3) The Addition Of Methyllithium To Give,After Reduction Of The Intermediate Diol 23 With Sodium Borohydride,The Target Ring System. In This Fashion,Ellipticine (1A),9-Methoxyellipticine (1B),And 9-Hydroxyellipticine (1C) Were Synthesized In Excellent Overall Yields From Indole. The Use Of Superhydride,In Place Of 1 Equiv Of Methyllithium,Provided A Synthesis Of Olivacine (2),And The Use Of Phthalic Anhydride In The Sequence Allowed For The Preparation Of 6,11-Dimethylbenzo[b]Carbazole (48). The Overall Yields Of Ellipticine (1A) (54%) And 9-Methoxyellipticine (1B) (47%) In Six Steps From Their Respective Indoles Represent One Of The Most Efficient Syntheses Of These Antitumor Alkaloids.
Doi:10.1021/jo00048A022

专利信息

专利号:US-7956011-B2
优先权日:2005-05-04
标题:Materials and methods for the photodirected synthesis of oligonucleotide arrays
发明人：SERAFINOWSKI PAWEL JERZY; GARLAND PETER BRYAN
权利人:CANCER RES INST ROYAL
摘要:Materials and methods for photodirected synthesis of oligonucleotide arrays on a solid substrate by photodirected synthesis are disclosed which employ a film formed from (i) a photoacid generator that on photolysis generates acid that is capable of directly removing the protecting group of the linker molecules or oligonucleotides and (ii) a polymer substantially lacking electronegative heteroatoms that are capable of hydrogen bonding with photogenerated acid. Methods of synthesizing an oligomer arrays are also described that use a film that restricts diffusion of reactants and products on the substrate during synthesis of the array and which includes a precursor of a deprotecting reagent. The method involves removing one or more of the non-required products of the deprotection reaction from the reactive array elements at which they are produced during the reaction, in order to displace the deprotection reaction towards completion.

专利号:US-9969686-B2
优先权日:2014-08-05
标 题 :Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
发明人：TANG WEIPING; LI XIAOXUN; SHU DONGXU; WINSTON-MCPHERSON GABRIELLE N
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.

专利号:US-2008280855-A1
优先权日:2005-06-22
标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles
发明人：CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO
权利人:NYCOMED GMBH
摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.

专利号:US-6448412-B1
优先权日:1995-07-31
标题:Methods for the preparation and characterization of multi-substituted fullerenes
发明人：MURPHY RANDALL B; WILSON STEPHEN R; LU QUING
权利人:SPHERE BIOSYSTEMS INC
摘要:The invention is directed to multiply-substituted fullerene derivatives of novel configurations, and methods for their preparation and use. The methods involve the combinatorial synthesis of a library of fullerene derivatives and comprises the steps of forming a mixture of fullerene derivatives by reacting the C n fullerene with two or more reactive precursor compounds, and removing the unreacted compounds to yield the fullerene derivatives having the desired activity. Methods for the identification and screening of a combinatorial library of fullerenes by 3 He-nuclear magnetic resonance and electrospray mass spectrometry to define members with the optimal desired activity are also provided.

专利号:WO-2007141253-A1
优先权日:2006-06-07
标 题 :Process for the production of intermediates for the preparation of tricyclic imidazopyridines
发明人：PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO
权利人:NYCOMED GMBH; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO
摘要:The invention relates to a process for the synthesis of compounds of the formula (1-a) and compounds of the formula (1-b). The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Arom have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.

专利号:WO-2010008727-A1
优先权日:2008-06-16
标 题:Asymmetric synthesis of allyl or allene oxindoles
发明人：KOZLOWSKI MARISA C; LINTON ELIZABETH CAROL
权利人:UNIV PENNSYLVANIA; KOZLOWSKI MARISA C; LINTON ELIZABETH CAROL
摘要:The invention concerns processes for the preparation of a compound of the formula I comprising contacting a compound of formula II with a catalyst, said catalyst comprises (i) at least one of Pd and Cu and (ii) one or more of diamine, diphosphine and aminophosphine ligands; wherein Z is -C(R 5 )(R 6 )-C(R 2 )=C(R 3 )(R 4 ) and Y is -C(R 3 )(R 4 )-C(R 2 )=C(R 5 )(R 6 ) or Z is -C(R 5 )(R 6 )-C≡C-R 3 ; Y is or -C(R 3 )=C=C(R 5 )(R 6 ); X is NH, NR 15 , O or S; a is O or an integer from 1 to 4 and R 1 -R 7 and R 15 are as defined in the specification.