- Process Optimization for the Large-Scale Preparation of (2 S,3 aR,7 aS)- tert-Butyl Hexahydro-2,5-methanopyrrolo[3,2- c]pyridine-1(4 H)-carboxylate, an Intermediate for Nicotinic Acetylcholine Receptor Agonists
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An optimized large-scale synthesis of (2S,3aR,7aS)-tert-butyl hexahydro-2,5-methanopyrrolo[3,2-c]pyridine-1(4H)-carboxylate (1A), an important intermediate for nicotinic acetylcholine receptor agonists, is described. The key feature of the synthesis involves three transformations in a one-pot process, including debenzylation and ring hydrogenation of two fused bicyclic rings. Multihundred gram quantities of 1A were prepared.
- Jarugu, Lokesh Babu,Reddy, China Anki,Chikkananjunda, Nanjundaswamy Kanikahalli,Krishnamoorthy, Suresh,Sarvanakumar, Pon,Sankar, Ulaganathan,Arunachalam, Pirama Nayagam,McDonald, Ivar M.,Olson, Richard E.,Rampulla, Richard,Mathur, Arvind,Gupta, Anuradha
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- Palladium-catalyzed synthesis of 2,3-disubstituted 5-azaindoles via heteroannulation reaction and of 2-substituted 5-azaindoles through domino sila-Sonogashira/5-endo cyclization
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A general and efficient procedure for the synthesis of 2,3-disubstituted 5-azaindoles through the palladium-catalyzed heteroannulation of 4-acetamido-3-iodopyridines and diaryl-, dialkyl-, or arylalkylalkynes is described along with a study of the reactio
- Livecchi, Marion,Calvet, Geraldine,Schmidt, Frederic
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experimental part
p. 5006 - 5016
(2012/07/03)
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- TETRACYCLIC INHIBITORS OF JANUS KINASES
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The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.
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Page/Page column 96
(2008/06/13)
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