CAS: 1076-74-0; 5-Methoxy-2-Methyl-1H-Indole

相似化合物

1968-13-4 21778-81-4 13314-85-7

上下游产品

5-甲氧基吲哚 5-Methoxylindole 1006-94-6
2-Bromo-5-Methoxy-1H-Indole 169383-96-4
2-Methyl-3-Methylthio-5-Methoxy-1H-Indole 50461-37-5
5-Methoxy-2-Methyl-3-(Phenylthio)-1H-Indole 98055-12-0
5-甲氧基-2-甲基-1H-吲哚-3-羧酸 5-Methoxy-2Methyl-1H-Indole-3-Carboxylic Acid 32387-22-7

1-(苯磺酰基)-5-甲氧基吲哚置于正丁基锂,Sodium Hydroxide体系中,用 四氢呋喃,乙醇,水 用作溶剂,化学反应生成5-甲氧基-2-甲基吲哚
参考文献:Discovery Of A First-In-Class,Potent,Selective,And Orally Bioavailable Inhibitor Of The P97 Aaa Atpase (Cb-5083)
标题:Discovery Of A First-In-Class,Potent,Selective,And Orally Bioavailable Inhibitor Of The P97 Aaa Atpase (Cb-5083)
摘要:The Aaa-Atpase P97 Plays Vital Roles In Mechanisms Of Protein Homeostasis,Including Ubiquitin Proteasome System (Ups) Mediated Protein Degradation,Endoplasmic Reticulum-Associated Degradation (Brad),And Autophagy. Herein We Describe Our Lead Optimization Efforts Focused On In Vitro Potency,Adme,And Pharmaceutical Properties That Led To The Discovery Of A Potent,Atp-Competitive,D2-Selective,And Orally Bioavailable P97 Inhibitor 71,Cb-6083. Treatment Of Tumor Cells With 71 Leads To Significant Accumulation Of Markers Associated With Inhibition Of Ups And Erad Functions,Which Induces Irresolvable Proteotoxic Stress And Cell,Death. In Tumor Bearing Mice,Oral Administration Of 71 Causes Rapid Accumulation Of Markers Of The Unfolded Protein Response (Upr) And Subsequently Induces Apoptosis Leading To Sustained Antitumor Activity In In Vivo,Xenograft Models Of Both Solid And Hematological Tumors. 71 Has Been Taken Into Phase I Clinical Trials In Patients With Multiple Myeloma And Solid Tumors.
Doi:10.1021/acs.Jmedchem.5B01346

专利信息

专利号:US-6531477-B1
优先权日:1998-10-13
标 题:6-substituted pyrazolo [3,4-d] pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
发明人：MARKWALDER JAY A; SEITZ STEVEN P; SHERK SUSAN R
权利人:DU PONT PHARM CO
摘要:The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T.This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

专利号:US-6559152-B2
优先权日:1998-10-13
标 题 :6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
发明人：MARKWALDER JAY A; SEITZ STEVEN P; SHERK SUSAN R
权利人:DU PONT PHARM CO
摘要:The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T.This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

专利号:US-9334275-B2
优先权日:2011-12-19
标题:Processes for preparing indoles
发明人：YOSHIKAI NAOHIKO; WEI YE
权利人:UNIV NANYANG TECH
摘要:Methods for the synthesis of an indole in provided. Methods comprise oxidizing a N-aryl imine in the presence of a palladium-based catalyst, an oxidant, and a solvent.

专利号:US-2021198197-A1
优先权日:2019-12-03
标题:Method for synthesizing indomethacin and analogue thereof
发明人：CHEN ZHILONG; LU HELIN
权利人:UNIV HUAZHONG SCIENCE TECH
摘要:The present disclosure belongs to the technical field of indomethacin synthesis, and discloses a method for synthesizing an indomethacin and an analogue thereof. The method for synthesizing an indomethacin and an analogue thereof includes steps of: introducing an alkyl group, an aromatic ring or a heteroaromatic ring directly at the C2 position of indole, a carboxylic acid fragment at the C3 position of the indole, and an aroyl group at the N1 position of the indole through palladium-catalyzed reactions. The present disclosure solves a problem: most of the existing indomethacin synthesis methods are achieved by construction of an indole ring and modification; simple structural changes of an indomethacin molecule based on this synthetic strategy often require de novo synthesis; the late modification and structure-activity relationship study of the indomethacin molecule have lengthy synthetic steps.

专利号:US-4160862-A
优先权日:1972-06-12
标 题 :1-Acyl-3-(amino-lower-alkyl)indoles
发明人：ZENITZ BERNARD L
权利人:STERLING DRUG INC
摘要:1-Acyl-3-(amino-lower-alkyl)indoles, useful as anti-inflammatory agents, are prepared either by acylation of a 3-(amino-lower-alkyl)indole; by Fisher indole synthesis from an N'-acylphenylhydrazine and an amino-lower-alkanone; by alkylation of an amine with a 1-acyl-3-(halo-lower-alkyl)indole; or by reductive alkylation of a 1-acyl-3-indole-lower-alkylcarboxaldehyde.

专利号:RU-2151148-C1
优先权日:1994-04-22
标 题:3-indolylpiperidines, method of their synthesis, pharmaceutical composition and method of its preparing