126781-38-2Relevant articles and documents
Selenium analogues of (S)-clopidogrel: Preparation method and properties
Vasiljeva, Jelena,Domracheva, Ilona,Arsenyan, Pavel
, p. 196 - 198 (2016)
A simple approach to prepare selenium containing analogues of (S)-clopidogrel using selenophene ring construction was developed. Evaluation of the antiproliferative activity profile confirmed that the introduction of a selenium atom into the molecule of c
Cyclic Alkenylsulfonyl Fluorides: Palladium-Catalyzed Synthesis and Functionalization of Compact Multifunctional Reagents
Lou, Terry Shing-Bong,Bagley, Scott W.,Willis, Michael C.
supporting information, p. 18859 - 18863 (2019/11/19)
A series of low-molecular-weight, compact, and multifunctional cyclic alkenylsulfonyl fluorides were efficiently prepared from the corresponding alkenyl triflates. Palladium-catalyzed sulfur dioxide insertion using the surrogate reagent DABSO effects sulfinate formation, before trapping with an F electrophile delivers the sulfonyl fluorides. A broad range of functional groups are tolerated, and a correspondingly large collection of derivatization reactions are possible on the products, including substitution at sulfur, conjugate addition, and N-functionalization. Together, these attributes suggest that this method could find new applications in chemical biology.
Nickel-Catalyzed Decarboxylative Alkenylation of Anhydrides with Vinyl Triflates or Halides
Chen, Hui,Sun, Shuhao,Liao, Xuebin
supporting information, p. 3625 - 3630 (2019/05/24)
Decarboxylative cross-coupling of aliphatic acid anhydrides with vinyl triflates or halides was accomplished via nickel catalysis. This methodology works well with a broad array of substrates and features abundant functional group tolerance. Notably, our approach addresses the issue of safe and environmental installation of methyl or ethyl group into molecular scaffolds. The method possesses high chemoselectivity toward alkyl groups when aliphatic/aromatic mixed anhydrides are involved. Furthermore, diverse ketones could be modified with our strategy.
A MODIFIED PROCESS FOR THE PREPARATION OF CERITINIB AND AMORPHOUS FORM OF CERITINIB
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Page/Page column 15, (2017/10/18)
The present invention is related to an improved process for the preparation of ceritinib with high yield and high purity. The present process is cost effective and feasible in large scale production also. The present invention also related to a stable amorphous form of ceritinib and its preparation. The present invention also relates to a process for the preparation of Crystalline form A of Ceritinib.
VMAT INHIBITORY COMPOUNDS
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Paragraph 0433-0435, (2016/04/01)
Disclosed herein are compounds that bind to the vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions comprising those compounds, and methods of treatment using said compounds and pharmaceutical compositions.
SUBSTITUTED 2-AZA-BICYCLO[2.2.1]HEPTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C
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Paragraph 0604 - 0607; 0608, (2014/09/29)
This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
A strategy for isotope containment during radiosynthesis - Devolatilisation of bromobenzene by fluorous-tagging-Ir-catalysed borylation en route to the 4-phenylpiperidine pharmacophore
Spivey, Alan C.,Martin, Laetitia J.,Tseng, Chih-Chung,Ellames, George J.,Kohler, Andrew D.
supporting information; experimental part, p. 4093 - 4095 (2009/02/07)
Syntheses of two 4-phenylpiperidines from bromobenzene have been developed involving anchoring to a fluorous-tag, Ir-catalysed borylation, Pd- and Co-catalysed elaboration then traceless cleavage. Although performed using 'cold' (i.e. unlabelled) bromoben
N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
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Page/Page column 20, (2010/11/30)
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
Terminal Heck vinylations of chelating vinyl ethers
Stadler, Alexander,Von Schenck, Henrik,Vallin, Karl S. A.,Larhed, Mats,Hallberg, Anders
, p. 1773 - 1781 (2007/10/03)
Terminal chelation-controlled Heck vinylations of electron-rich amino-functionalized vinyl ethers were performed with high regioselectivity furnishing moderate to good isolated yields of the corresponding 1-alkoxy-1,3-butadienes. DFT calculations support
Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5′-sulfonamide moiety of phenyl ring
Kim, Dae-Kee,Lee, Ju Young,Park, Hyun-Ju,Thai, Khac Minh
, p. 2099 - 2103 (2007/10/03)
Synthesis of new sildenafil analogues containing a phosphonate group in the 5′-sulfonamide moiety of the phenyl ring, 12a-e, 13a-d, and 14a-d, and evaluation of their in vitro PDE5 inhibitory activity are disclosed. Enzyme assays revealed that