150869-52-6Relevant academic research and scientific papers
LINCOMYCIN DERIVATIVES AND ANTIBACTERIAL AGENTS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
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Page/Page column 39, (2010/03/02)
An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R1 represents N-optionally substituted C1-6 alkyl-N-optionally substituted C1-6 alkylamino-C1-6 alkyl; R2 represents a hydrogen atom or optionally substituted C1-6 alkyl; R3 represents optionally substituted C1-6alkyl or C3-6 cycloalkyl-C1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.
Preparative fluorous mixture synthesis of diazonium-functionalized oligo(phenylene vinylene)s
Jian, Huahua,Tour, James M.
, p. 3396 - 3424 (2007/10/03)
(Chemical Equation Presented) A series of building blocks for the synthesis of oligo(phenylene vinylene)s (OPVs) and hybrid oligomers were prepared, and alternating Heck coupling and Horner-Wadswoth-Emmons (HWE) reactions were used to couple the building blocks. Model studies were carried out to optimize the reaction strategies. The products were made to bear aryl diazonium functionalities that allow them to be used as surface grafting moieties in hybrid silicon/molecule assemblies. A library of OPV and hybrid oligomer tetramers was synthesized using fluorous mixture synthesis (FMS). The fluorous tags, which are secondary amines bearing different numbers of fluorine atoms, were synthesized and used as phase tags in mixture synthesis. The tags and substrates were anchored together by triazene linkages. The mixture synthesis was monitored by analytical HPLC on a fluorous column, and isolation of final OPV and hybrid oligomer tetramers was achieved by preparative HPLC. At the end of the FMS, after demixing, the tagged products were detagged by cleaving the triazene linkage and generating a series of aryl diazonium compounds. The fluorous tags could be recovered and reused. The NMR spectra of the 1-aryl-3,3-dialkyltriazenes are discussed.
Preparation of benzolactams by Pd(OAC)2-catalyzed direct aromatic carbonylation
Orito, Kazuhiko,Horibata, Akiyoshi,Nakamura, Takatoshi,Ushito, Harumi,Nagasaki, Hideo,Yuguchi, Motoki,Yamashita, Satoshi,Tokuda, Masao
, p. 14342 - 14343 (2007/10/03)
We developed a new method for Pd(II)-catalyzed direct aromatic carbonylation in a phosphine-free catalytic system using Pd(OAc)2 and Cu(OAc)2 in an atmosphere of CO gas containing air. The carbonylation proceeded with ortho-palladation, inducing a remarkable site selectivity to afford a variety of five- or six-membered benzolactams from secondary ω-arylalkylamines, such as N-alkylbenzylamines or N-alkylphenethylamines. Copyright
Process for the preparation of tetrazoles
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, (2008/06/13)
The present invention relates to a process for the preparation of 5-aryl tetrazoles of the formula: STR1 or a salt thereof comprising reacting an aryl nitrile with a trisubstituted silyl azide and a disubstituted tin oxide.
An efficient synthesis of an angiotensin II antagonist (A-81988)
Kerdesky,Haight,Narayanan,Nordeen,Scarpetti,Seif,Wittenberger,Morton
, p. 2027 - 2039 (2007/10/02)
A new and efficient synthesis of A-81988, an angiotensin II antagonist, is described. The preparation utilizes a novel method for tetrazole formation from nitriles requiring trimethylsilyl azide and a catalytic amount of dialkyltin oxide.
1,3-oxazolyl substituted biphenyl
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, (2008/06/13)
The present invention relates to a process for the preparation of a compound of the formula: STR1 wherein R1 is selected from the group consisting of hydrogen, loweralkyl, loweralkoxy-substituted loweralkyl, lower alkenyl, lower alkynyl, cycloalkyl and cycloalkylalkyl; R2 is selected from the group consisting of hydrogen, loweralkyl, loweralkoxy-substituted loweralkyl, halogen and loweralkoxy; R3 is selected from hydrogen, loweralkyl, and halogen; R* and R** are independently selected from loweralkyl and P1 is hydrogen or an nitrogen-protecting group; or an acid addition salt thereof.
