188867-89-2Relevant articles and documents
Highly Enantioselective Iridium-Catalyzed Coupling Reaction of Vinyl Azides and Racemic Allylic Carbonates
Han, Min,Yang, Min,Wu, Rui,Li, Yang,Jia, Tao,Gao, Yuanji,Ni, Hai-Liang,Hu, Ping,Wang, Bi-Qin,Cao, Peng
, p. 13398 - 13405 (2020/09/02)
The iridium-catalyzed enantioselective coupling reaction of vinyl azides and allylic electrophiles is presented and provides access to β-chiral carbonyl derivatives. Vinyl azides are used as acetamide enolate or acetonitrile carbanion surrogates, leading to γ,δ-unsaturated β-substituted amides as well as nitriles with excellent enantiomeric excess. These products are readily transformed into chiral N-containing building blocks and pharmaceuticals. A mechanism is proposed to rationalize the chemoselectivity of this coupling reaction.
Evolution of a Scale-Up Synthesis to a Potent GluN2B Inhibitor and Its Prodrug
Kempson, James,Zhang, Huiping,Wong, Michael K. Y.,Li, Jianqing,Li, Peng,Wu, Dauh-Rurng,Rampulla, Richard,Galella, Michael A.,Dabros, Marta,Traeger, Sarah C.,Muthalagu, Vetrichelvan,Gupta, Anuradha,Arunachalam, Pirama Nayagam,Mathur, Arvind
, p. 846 - 855 (2018/06/13)
This paper describes the efficient scale-up synthesis of the potent negative allosteric glutamate N2B (GluN2B) inhibitor 1 (BMS-986169), which relies upon a stereospecific SN2 alkylation strategy and a robust process for the preparation of its
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder
Marcin, Lawrence R.,Warrier, Jayakumar,Thangathirupathy, Srinivasan,Shi, Jianliang,Karageorge, George N.,Pearce, Bradley C.,Ng, Alicia,Park, Hyunsoo,Kempson, James,Li, Jianqing,Zhang, Huiping,Mathur, Arvind,Reddy, Aliphedi B.,Nagaraju,Tonukunuru, Gopikishan,Gupta, Grandhi V. R. K. M.,Kamble, Manjunatha,Mannoori, Raju,Cheruku, Srinivas,Jogi, Srinivas,Gulia, Jyoti,Bastia, Tanmaya,Sanmathi, Charulatha,Aher, Jayant,Kallem, Rajareddy,Srikumar, Bettadapura N.,Vijaya, Kumar Kuchibhotla,Naidu, Pattipati S.,Paschapur, Mahesh,Kalidindi, Narasimharaju,Vikramadithyan, Reeba,Ramarao, Manjunath,Denton, Rex,Molski, Thaddeus,Shields, Eric,Subramanian, Murali,Zhuo, Xiaoliang,Nophsker, Michelle,Simmermacher, Jean,Sinz, Michael,Albright, Charlie,Bristow, Linda J.,Islam, Imadul,Bronson, Joanne J.,Olson, Richard E.,King, Dalton,Thompson, Lorin A.,Macor, John E.
supporting information, p. 472 - 477 (2018/05/23)
There is a significant unmet medical need for more efficacious and rapidly acting antidepressants. Toward this end, negative allosteric modulators of the N-methyl-d-aspartate receptor subtype GluN2B have demonstrated encouraging therapeutic potential. We
Selective NR2B Antagonists
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Paragraph 0368, (2015/07/15)
The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the c
(R)-3-((3S,4S)-3-FLUORO-4-(4-HYDROXYPHENYL)PIPERIDIN-1-YL)-1-(4-METHYLBENZYL)PYRROLIDIN-2-ONE AND ITS PRODRUGS FOR THE TREATMENT OF PSYCHIATRIC DISORDERS
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, (2015/07/15)
The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the NR2B NMDA receptor and may be useful for the treatment of various disorders of
Piperidine derivatives having renin inhibiting activity
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, (2008/06/13)
Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I wherein R1, R2, R3, R4, Q, X, Z, m and n are as described herein.
