CAS: 5198-88-9; 2-Bromothiazole-4-Carboxylic Acid

上下游产品

CAS号100367-77-9 2-溴噻唑-4-甲酸乙酯 | CAS号170235-26-4 2-溴噻唑-4-羧酸甲酯 | CAS号83553-47-3 2-Iodo-thiazole... | CAS号848501-94-0 2-溴噻唑-4-甲酰胺

2-溴噻唑-4-甲酸乙酯置于potassium Carbonate体系中,用 甲醇,水 作为反应溶剂,化学反应 3.0H,以99%的收率获得产物2-溴-4-噻唑羧酸
参考文献:噻唑基肽抗生素ge2270 A的简明全合成.
标题:噻唑基肽抗生素ge2270 A的简明全合成.
摘要:由n-叔丁氧羰基保护的缬氨酸以最长的20步线性序列合成了有效的抗生素噻唑基肽ge2270 A,总产率为4.8%.关键策略是通过从2,6-二溴-3-碘吡啶开始的连续交叉偶联反应组装2,3,6-三取代吡啶核.通过3-锌的2,6-二溴吡啶的negishi交叉偶联将完整的southern片段安装在三噻唑的2-碘噻唑末端(87%).在通过另一个negishi交叉偶联金属化成锌试剂后,以截短的2-溴噻唑-4-羧酸叔丁酯形式引入代表分子北部的c-6处的取代基.整个序列的决定性步骤是将大环化成29元大环内酰胺,这是通过发生在吡啶核的c-2处的分子内stille交叉偶联进行的,以75%的收率提供所需的产物.通过在代表ge2270 A东部的复杂二噻唑片段与3,6-二取代的2-溴吡啶之间的酰胺键形成(87%)获得所需的锡烷.最终步骤包括将丝氨酸-脯氨酸酰胺二肽附着到分子的北部(65%),形成恶唑啉环和甲硅烷基醚脱保护(总体占55%).
DOI:10.1002/chem.200701823

专利信息

专利号:US-2010047841-A1
优先权日:2007-02-27
标 题 :Synthesis of desacetoxytubulysin h and analogs thereof
发明人：WIPF PETER; WANG ZHIYONG
权利人:UNIV PITTSBURGH
摘要:Compounds of formula I, XVI and XXI possess potent cell growth inhibitory activity. These compounds are described have therapeutic utility, particularly in the treatment of cancer as well as conditions and disorders related to uncontrolled cell growth: n n n n n n n n n n wherein the variables R 1 , R 2 , R 3 , R 4 , R 5 , X, Y and Z are described herein.

专利号:EP-3686190-A1
优先权日:2013-07-11
标 题 :Synthesis of therapeutically active compounds

专利号:US-2022204495-A1
优先权日:2019-05-03
标题:Inhibiting trabid
发明人：CAMPBELL ANNE-MARIE; MARCIN Lawrence; KAYSER-BRICKER KATHERINE
权利人:VALO HEALTH INC; INTEGRAL HEALTH HOLDINGS LLC
摘要:The present disclosure is directed to compounds of formulas (I)-(VII), which are useful as modulators of TRABID. The compounds are further useful in the inhibition of TRABID and the treatment of diseases or disorders associated with the inhibition of TRABID. For instance, the disclosure is concerned with compounds and compositions for inhibition of TRABID, methods of treating diseases associated with the inhibition of TRABID (e.g., autoimmune inflammatory diseases including, but not limited to, psoriasis), and methods of synthesis of these compounds.

专利号:WO-2008106080-A9
优先权日:2007-02-27
标题 :Synthesis of desacetoxytubulysin h and analogs thereof

专利号:WO-2008106080-A2
优先权日:2007-02-27
标 题 :Synthesis of desacetoxytubulysin h and analogs thereof

专利号:WO-2014024119-A1
优先权日:2012-08-06
标 题:Heterocyclic amides as itk inhibitors
发明人：KUMAR SUKEERTHI; THOMAS ABRAHAM; CHIKHALE RAJENDRA PRAKASH; WAGHMARE NAYAN TATERAO; KADLAG NANASAHEB; KHAIRATKAR-JOSHI NEELIMA; SHAH DAISY MANISH
权利人:GLENMARK PHARMACEUTICALS SA
摘要:The present invention is directed to heterocyclic amide compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by ITK.