449811-20-5Relevant articles and documents
Selective Reductive Elimination at Alkyl Palladium(IV) by Dissociative Ligand Ionization: Catalytic C(sp3)?H Amination to Azetidines
Nappi, Manuel,He, Chuan,Whitehurst, William G.,Chappell, Ben G. N.,Gaunt, Matthew J.
supporting information, p. 3178 - 3182 (2018/02/28)
A palladium(II)-catalyzed γ-C?H amination of cyclic alkyl amines to deliver highly substituted azetidines is reported. The use of a benziodoxole tosylate oxidant in combination with AgOAc was found to be crucial for controlling a selective reductive elimination pathway to the azetidines. The process is tolerant of a range of functional groups, including structural features derived from chiral α-amino alcohols, and leads to the diastereoselective formation of enantiopure azetidines.
6,7-DIHYDRO-4H-PYRAZOLO[1,5-A]PYRAZINE COMPOUNDS FOR THE TREATMENT OF INFECTIOUS DISEASES
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Page/Page column 36-37, (2018/03/26)
The present invention relates to compounds of the formula (I) or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R4 are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.
3-amido pyrrolopyrazine JAK kinase inhibitors: Development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models
Soth, Michael,Hermann, Johannes C.,Yee, Calvin,Alam, Muzaffar,Barnett, Jim W.,Berry, Pamela,Browner, Michelle F.,Frank, Karl,Frauchiger, Sandra,Harris, Seth,He, Yang,Hekmat-Nejad, Mohammad,Hendricks, Than,Henningsen, Robert,Hilgenkamp, Ramona,Ho, Hoangdung,Hoffman, Ann,Hsu, Pei-Yuan,Hu, Dong-Qing,Itano, Andrea,Jaime-Figueroa, Saul,Jahangir, Alam,Jin, Sue,Kuglstatter, Andreas,Kutach, Alan K.,Liao, Cheng,Lynch, Stephen,Menke, John,Niu, Linghao,Patel, Vaishali,Railkar, Aruna,Roy, Douglas,Shao, Ada,Shaw, David,Steiner, Sandra,Sun, Yongliang,Tan, Seng-Lai,Wang, Sandra,Vu, Minh Diem
supporting information, p. 345 - 356 (2013/02/23)
The Janus kinases (JAKs) are involved in multiple signaling networks relevant to inflammatory diseases, and inhibition of one or more members of this class may modulate disease activity or progression. We optimized a new inhibitor scaffold, 3-amido-5-cycl
Enantioselective preparation of P-chiral phosphine oxides
Adams, Harry,Collins, Rebecca C.,Jones, Simon,Warner, Christopher J. A.
supporting information; experimental part, p. 6576 - 6579 (2012/01/15)
A highly efficient chiral auxiliary-based strategy for the asymmetric synthesis of P-chiral phosphine oxides in >98:2 er has been developed. The methodology involves the highly stereoselective formation of P-chiral oxazolidinones that then undergo displacement with a variety of Grignard reagents to prepare the desired phosphine oxides.
PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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Page/Page column 46, (2010/08/18)
The present application describes modulators of MIP-1α of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.
CYCLIC UREA INHIBITORS OF HB-HYDROXYSTEROID DEHYDROGENASE 1
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Page/Page column 60, (2009/07/17)
This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell Or the inhibition of the conversion of cortisone to Cortisol in a cell.
PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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Page/Page column 130-131, (2009/03/07)
The present application describes modulators of MIP-1 of formula (I) : or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.
A practical procedure for the multigram synthesis of the SuperQuat chiral auxiliaries
Bull, Steven D.,Davies, Stephen G.,Jones, Simon,Polywka, Mario E. C.,Shyam Prasad,Sanganee, Hitesh J.
, p. 519 - 521 (2007/10/03)
An efficient and simple synthesis of oxazolidin-2-one SuperQuat chiral auxiliaries is described which provides rapid access to multigram quantities of the auxiliaries.