CAS: 59-49-4; Benzo[d]Oxazol-2(3H)-One

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22876-15-9 22876-16-0 19932-85-5

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水杨基羟肟酸置于氯化亚砜体系中,化学反应生成 2-苯并唑啉酮
参考文献:3,3'-(苯基亚膦基)双[2(3H)-苯并恶唑酮]和3,3'-(苯基亚膦基)双[2(3H)-苯并噻唑酮].新活化剂
标题:3,3'-(苯基亚膦基)双[2(3H)-苯并恶唑酮]和3,3'-(苯基亚膦基)双[2(3H)-苯并噻唑酮].新活化剂
摘要:新的活化剂 3,3'-(苯基亚膦基)双 [2(3H)-苯并恶唑酮] (4) 和 3,3'-(苯基亚膦基)双[2(3H)-苯并噻唑酮] (5) 可以通过以下方式轻松制备在室温下,在三乙胺存在下,苯基膦酰二氯 (3) 分别与 2(3H)-苯并恶唑酮 (1) 和 2(3H)-苯并噻唑酮 (2) 反应.发现新的活化剂 4 和 5 可用于在温和条件下制备酰胺,酯和二肽.此外,间苯二甲酸与芳族二胺在吡啶存在下使用活化剂 4 的直接缩聚反应在室温下快速进行,以产生特性粘度高达 0.80 Dl/g 的聚酰胺.
DOI:10.1246/bcsj.58.3291

专利信息

专利号:US-2004018598-A1
优先权日:2000-05-30
标题 :Bio-intermediates for use in the chemical synthesis of polyketides
发明人：SANTI DANIEL; ASHLEY GARY; MYLES DAVID C
摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.

专利号:US-11542269-B2
优先权日:2018-01-03
标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof
发明人：CHOI HYEONG-WOOK; FANG FRANCIS G
权利人:EISAI R&D MAN CO LTD
摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.

专利号:WO-2012047907-A9
优先权日:2010-10-04
标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto
发明人：MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.

专利号:US-10913749-B2
优先权日:2015-05-07
标 题 :Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides
发明人：FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E
权利人:EISAI R&D MAN CO LTD
摘要:The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.

专利号:US-11136335-B2
优先权日:2016-06-30
标题:Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof
发明人：CHASE CHARLES E; CHOI HYEONG-WOOK; ENDO ATSUSHI; FANG FRANCIS G; KIM DAE-SHIK
权利人:EISAI R&D MAN CO LTD
摘要:The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.

专利号:US-12240835-B2
优先权日:2018-09-18
标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity
发明人：ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI
权利人:TERNS PHARMACEUTICALS INC
摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.