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CAS号2302-25-2 4-溴-1H-咪唑 | CAS号74-88-4 碘甲烷 | CAS号1003-50-5 4,5-二溴-1-甲基-1H-咪唑 | CAS号1003-91-4 2,4,5-三溴-1-甲基-1H-咪唑 | CAS号77-78-1 硫酸二甲酯合成工艺路线路线简述
- 合成目标产物 4-Bromo-1-Methyl-1H-Imidazole 主要起始原料 2,4,5-Tribromo-1-Methyl-1H-Imidazole
- (文献来源)合成步骤主要原料 2,4,5-Tribromo-1-Methyl-1H-Imidazole
4,5-二溴-1-甲基-1H-咪唑置于正丁基锂体系中,用 乙醚 用作溶剂,以80%的收率获得4-溴-1-甲基-1H-咪唑
参考文献:Borai,M. El; Moustafa,A. H.; Anwar,M.,Polish Journal Of Chemistry,1981,Vol. 55,# 7/8,P. 1659-1665
标题:Borai,M. El; Moustafa,A. H.; Anwar,M.,Polish Journal Of Chemistry,1981,Vol. 55,# 7/8,P. 1659-1665
专利信息
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: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-2023091726-A1
优先权日:2021-11-18
标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12)
发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH
权利人:SYROS PHARMACEUTICALS INC
摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:US-9879022-B2
优先权日:2014-04-04
标题:Bicyclic-fused heteroaryl or aryl compounds
发明人:TRZUPEK JOHN DAVID; LEE KATHERINE LIN; BUNNAGE MARK EDWARD; HAN SEUNGIL; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; PAPAIOANNOU NIKOLAOS; PIERCE BETSY SUSAN; STROHBACH JOSEPH WALTER; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG; GAVRIN LORI KRIM; LEE ARTHUR; ANDERSON DAVID RANDOLPH; CURRAN KEVIN JOSEPH; DEHNHARDT CHRISTOPH MARTIN; SAIAH EDDINE; GOLDBERG JOEL ADAM; WANG XIAOLUN; HUANG HORNG-CHIH; VARGAS RICHARD; LOWE MICHAEL DENNIS; PATNY AKSHAY
权利人:PFIZER
摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9795613-B2
优先权日:2014-12-10
标题 :GLP-1 receptor modulators
发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL; GLYNN DANIEL; MILLS MARK
权利人:CELGENE INT II SÀRL
摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.
专利号:US-9187522-B2
优先权日:2011-12-12
标题 :GLP-1 receptor modulators
发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL
权利人:RECEPTOS INC
摘要:The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.