CAS: 763120-43-0; 2-Pyrrolylboronic Acid

1-(苯基磺酰基)吡咯置于异丙基溴化镁,二异丙胺,硼酸三甲酯体系中,用 四氢呋喃 作为反应溶剂,化学反应 16.0H,以13%的收率获得产物2-吡咯硼酸
参考文献:使用格氏试剂和催化胺的镁化作用.在n-苯基磺酰基吡咯的功能化中的应用.
标题:使用格氏试剂和催化胺的镁化作用.在n-苯基磺酰基吡咯的功能化中的应用.
摘要:[反应:见正文] N-苯基磺酰基吡咯1通过用异丙基氯化镁和催化二异丙胺处理而被镁化.与各种亲电试剂反应,包括钯催化的芳基和杂芳基交叉偶联,可以中等至非常好的产率提供2-取代的苯磺酰基吡咯.
DOI:10.1021/ol036288P

专利信息

专利号:US-8207337-B2
优先权日:2007-01-29
标 题:Reagent for organic synthesis reaction containing organic triol borate salt
发明人：MIYAURA NORIO; YAMAMOTO YASUNORI
权利人:MIYAURA NORIO; YAMAMOTO YASUNORI; WAKO PURE CHEM IND LTD
摘要:[Problem] n To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. n [Means for Solving Problems] n The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R 1 represents alkyl, alkenyl, etc.; R 2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m + represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M 2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).

专利号:US-7612064-B2
优先权日:2003-05-26
标题:Sulfopyrroles
发明人：EBERLE MARTIN; ERMERT PHILIPP; OBRECHT DANIEL; LACH FRANK; LUTHER ANATOL; BACHMANN FELIX; STREBEL ALLESSANDRO
权利人:TAKEDA PHARMACEUTICAL
摘要:The invention relates to compounds of formula (I) wherein R 1 represents aryl, aralkyl or heteroaryl, R 2 is aryl or heteroaryl and R 3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.

专利号:WO-2014041518-A1
优先权日:2012-09-14
标题:Thienopyrrole derivatives as itk inhibitors
发明人：KUMAR SUKEERTHI; THOMAS ABRAHAM; KHAIRATKAR-JOSHI NEELIMA; SHAH DAISY MANISH
权利人:GLENMARK PHARMACEUTICALS SA
摘要:The present invention is directed to thienopyrrole 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.