- Interrupting the Barton?McCombie reaction: Aqueous deoxygenative trifluoromethylation of o-alkyl thiocarbonates
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The site-selective trifluoromethylation of aliphatic systems remains an important challenge. This work describes a light-driven, copper-mediated trifluoromethylation of O-alkyl thiocarbonates. The reaction provides broad functional group tolerance (e.g., alkyne, alkene, phenol, free alcohol, electron-rich and -deficient arenes), thereby offering orthogonality and practicality for trifluoromethylation. A radical organometallic mechanism is proposed.
- Liu, Zhi-Yun,Cook, Silas P.
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supporting information
p. 808 - 813
(2021/02/01)
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- HETEROBIFUNCTIONAL MOLECULES AS TEAD INHIBITORS
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The invention relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.
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Paragraph 0259-0260; 0398-0399
(2021/09/11)
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- Development of purine-derived 18F-labeled pro-drug tracers for imaging of MRP1 activity with PET
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Multidrug resistance-associated protein 1 (MRP1) is a drug efflux transporter that has been implicated in the pathology of several neurological diseases and is associated with development of multidrug resistance. To enable measurement of MRP1 function in
- Galante, Eva,Okamura, Toshimitsu,Sander, Kerstin,Kikuchi, Tatsuya,Okada, Maki,Zhang, Ming-Rong,Robson, Mathew,Badar, Adam,Lythgoe, Mark,Koepp, Matthias,?rstad, Erik
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p. 1023 - 1032
(2014/03/21)
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- RADIOHALOTHYMIDINES AND METHODS OF THEIR SYNTHESIS AND USE IN PET IMAGING OF CANCERS
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We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells. We also disclose specific N3 -radiohaloalkyl thymidines and salts thereof.
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Page/Page column 18
(2008/06/13)
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- Bismuth(III) chloride catalyzed efficient and selective cleavage of trityl ethers
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A highly selective and efficient protocol has been developed for detritylation using 5 mol% BiCl3 in acetonitrile. The cleavage proceeds at room temperature in high yields and the conditions are mild enough to tolerate a variety of acid-base sensitive functional groups.
- Sabitha, Gowravaram,Reddy, E. Venkata,Swapna,Reddy, N. Mallikarjun,Yadav
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p. 1276 - 1278
(2007/10/03)
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- Silver(I) oxide mediated highly selective monotosylation of symmetrical diols. Application to the synthesis of polysubstituted cyclic ethers
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(Matrix Presented) The reaction of symmetrical diols and oligo(ethylene glycol)s with a stoichiometric amount of p-toluenesulfonyl chloride in the presence of silver(I) oxide and a catalytic amount of potassium iodide led selectively to the monotosylate derivatives in high yields. Polysubstituted cyclic ethers were obtained readily upon treatment of the corresponding diols with an excess of silver oxide. The high selectivity was explained on the basis of the difference in acidity between the two hydroxy groups, which undergo an intramolecular hydrogen bonding.
- Bouzide, Abderrahim,Sauve, Gilles
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p. 2329 - 2332
(2007/10/03)
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- Facile and selective cleavage of allyl ethers, amines and esters using polymethylhydrosiloxane-ZnCl2/Pd(PPh3)4
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Allyl deprotection to liberate free hydroxy, amino and acid groups from the corresponding allyl ethers, amines and esters is achieved under mild conditions. The reagent combination employed for this transformation is polymethylhydrosiloxane (PMHS), ZnCl2 and Pd(PPh3)4.
- Chandrasekhar,Raji Reddy,Jagadeeshwar Rao
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p. 3435 - 3438
(2007/10/03)
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- Tetrabutylammonium tribromide (TBATB)-promoted tetrahydropyranylation/depyranylation of alcohols
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Alcohols are tetrahydropyranylated rapidly in high yields in the presence of a catalytic amount of TBATB in dichloromethane at room temperature. Depyranylation to their parent alcohol is achieved in quantitative yields by merely changing the solvent to methanol.
- Naik, Sarala,Gopinath, Rangam,Patel, Bhisma K
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p. 7679 - 7681
(2007/10/03)
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- Pyrimidine derivatives
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Pyrimidine derivatives useful as a gastrointestinal prokinetic agent, represented by formula STR1 wherein X is O or NR5, Y is O, S or NR5 wherein R5 is a hydrogen atom, a C1 -C6 alkyl group or the like; R1 and R2 may be the same or different and each is a hydrogen atom, a C1 -C6 alkyl group or the like; R3 is CN, or COOR6 wherein R6 is a C1 -C6 alkyl group, a C3 -C6 cycloalkyl group, an aryl group or the like; R4 is --SR7 or --NR8 R9 wherein R7 is a C1 -C6 alkyl group; R8 is a C1 -C6 alkyl group or the like; R9 is a hydrogen atom, a C1 -C6 alkyl group or the like, or R8 and R9 may represent, together with the nitrogen atom to which they are attached, an N-substituted piperazine ring of formula (X) STR2 wherein R10 represents a C1 -C6 alkyl group or the like or a pharmacologically acceptable salt thereof. The above-mentioned compounds are useful as a gastrointestinal prokinetic agent used for the therapy of digestive tract diseases.
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- 2-(acetoacetyloxy)-3-(octadecyloxy)propyl-3-trimethylammoniopropyl phosphate or a pharmaceutically acceptable salt thereof
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A compound provided by the present invention, of the formula STR1 wherein R1 is C14-20 alkyl; R2, R3 and R4 are independently hydrogen or C1-5 alkyl, or STR2 represents a cyclic ammonio gro
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