- Photo-auxiliary approach to control excited state reactivity: Cross [2+2]-photocycloaddition of oxazolidinone based hydrazides
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Chiral oxazolidinone based hydrazides undergo efficient cross [2 + 2]-photocycloaddition upon visible light illumination. Oxazolidinone functionality acted as an energy harvesting photo-auxiliary. The cross [2 + 2]-photocycloaddition proceeded efficiently from the excited state with moderate to excellent isolated yield of the photoproduct. The photo-auxiliary can be conveniently removed post-photoreaction, which highlights the versatility of this strategy.
- Ahuja, Sapna,Iyer, Akila,Kandappa, Sunil Kumar,Sivaguru, Jayaraman
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Read Online
- Development of a practical synthesis of a p38 kinase inhibitor via a safe and robust amination
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The development of a practical synthesis for a p38 kinase inhibitor is described. The key advances include an improved route to the key intermediate, a substituted pyrrole, and a subsequent animation utilizing O-(4-nitrobenzoyl)- hydroxylamine, which provides a safe, scalable, and robust amination method. The new protocol was successfully demonstrated to generate 1.6 kg of API in seven steps and 26% overall yield.
- Shi, Zhongping,Kiau, Susanne,Lobben, Paul,Hynes Jr., John,Wu, Hong,Parlanti, Luca,Discordia, Robert,Doubleday, Wendel W.,Leftheris, Katerina,Dyckman, Alaric J.,Wrobleski, Stephen T.,Dambalas, Konstantinos,Tummala, Srinivas,Leung, Simon,Lo, Ehrlic
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p. 1618 - 1625
(2013/02/23)
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- Fischer synthesis of isomeric thienopyrrole LHRH antagonists
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As part of a structure-activity exploration into LHRH antagonists, structures containing the thieno[2,3-b]pyrrole core were identified as potent antagonists. This letter describes the employment of the Fischer synthesis to access this thienopyrrole and isomeric final compounds.
- Andrews, David M.,Arnould, Jean-Claude,Boutron, Pascal,Délouvrie, Bénédicte,Delvare, Christian,Foote, Kevin M.,Hamon, Annie,Harris, Craig S.,Lambert-van der Brempt, Christine,Lamorlette, Maryannick,Matusiak, Zbegniew M.
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experimental part
p. 5805 - 5816
(2009/12/24)
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- KINESIN INHIBITORS
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This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat a kinesin Eg5 protein-mediated disorder.
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Page/Page column 63
(2009/01/20)
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- Amination of heterocyclic compounds with O-benzoylhydroxylamine derivatives
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The N-amination of heterocyclic compounds 1a - k with O- benzoylhydroxylamine derivatives 5 was developed and demonstrated to be a superior alternative to existing N-amination methods. A structure - reactivity relationship study was performed on variously
- Parlanti, Luca,Discordia, Robert P.,Hynes Jr., John,Miller, Michael M.,O'Grady, Harold R.,Shi, Zhongping
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p. 3821 - 3824
(2008/02/12)
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- Method for preparing pyrrolotriazine compounds
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A method for aminating pyrrole derivatives and for preparing pyrrolotriazine compounds having the formula V,
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Page/Page column 6-7
(2008/06/13)
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