6026-73-9Relevant academic research and scientific papers
Production of [...] (by machine translation)
-
Paragraph 0032, (2017/05/23)
Useful as an intermediate for the production of a horticultural [to] acaricidal agent can provide an industrially advantageous method for producing 3 - [...]. [Solution] nitro bromobenzene isobutene and the like, a palladium catalyst, a phosphine-based coordination, bases, solvents, and the auxiliary agent in the presence of reaction, isobutene was added to compound, the additional compound is isolated or not isolated, hydrogenation (catalytic reduction) by the production method 3 - [...] or salts thereof. [Drawing] no (by machine translation)
Cross-metathesis reaction of functionalized and substituted olefins using group 8 transition metal carbene complexes as metathesis catalysts
-
Page/Page column 36; 45, (2016/08/29)
The invention pertains to the use of Group 8 transition metal carbene complexes as catalysts for olefin cross-metathesis reactions. In particular, ruthenium and osmium alkylidene complexes substituted with an N-heterocyclic carbene ligand are used to catalyze cross-metathesis reactions to provide a variety of substituted and functionalized olefins, including phosphonate-substituted olefins, directly halogenated olefins, 1,1,2-trisubstituted olefins, and quaternary allylic olefins. The invention further provides a method for creating functional diversity using the aforementioned complexes to catalyze cross-metathesis reactions of a first olefinic reactant, which may or may not be substituted with a functional group, with each of a plurality of different olefinic reactants, which may or may not be substituted with functional groups, to give a plurality of structurally distinct olefinic products. The methodology of the invention is also useful in facilitating the stereoselective synthesis of 1,2-disubstituted olefins in the cis configuration.
Discovery of olodaterol, a novel inhaled β2-adrenoceptor agonist with a 24 h bronchodilatory efficacy
Bouyssou, Thierry,Hoenke, Christoph,Rudolf, Klaus,Lustenberger, Philipp,Pestel, Sabine,Sieger, Peter,Lotz, Ralf,Heine, Claudia,Büttner, Frank H.,Schnapp, Andreas,Konetzki, Ingo
scheme or table, p. 1410 - 1414 (2010/07/10)
Compound 4p was identified from a series of 6-hydroxy-4H-benzo[1,4]oxazin-3-ones as potent agonist of the human β2-adrenoceptor with a high β1/β2-selectivity. A complete reversal of acetylcholine-induced bronchoconstrictio
Synthesis of Symmetrical Trisubstituted Olefins by Cross Metathesis
Chatterjee, Arnab K.,Sanders, Daniel P.,Grubbs, Robert H.
, p. 1939 - 1942 (2007/10/03)
(Matrix Presented) Trisubstituted alkenes have been prepared via intermolecular olefin cross-metathesis (CM) between α-olefins and symmetrically 1,1-disubstituted olefins using an imidazolylidene ruthenium benzylidene complex. Of particular interest is th
Biphenylsulfonamide endothelin antagonists: Structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N-(3,4- dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1,1'-biphenyl]-2-sulfonamide (BMS- 187308)
Murugesan, Natesan,Gu, Zhengxiang,Stein, Philip D.,Bisaha, Sharon,Spergel, Steve,Girotra, Ravi,Lee, Ving G.,Lloyd, John,Misra, Raj N.,Schmidt, Joan,Mathur, Arvind,Stratton, Leslie,Kelly, Yolanda F.,Bird, Eileen,Waldron, Tom,Liu, Eddie C.-K.,Zhang, Rongan,Lee, Helen,Serafino, Randy,Abboa-Offei, Benoni,Mathers, Parker,Giancarli, Mary,Seymour, Andrea Ann,Webb, Maria L.,Moreland, Suzanne,Barrish, Joel C.,Hunt, John T.
, p. 5198 - 5218 (2007/10/03)
Substitution at the ortho position of N-(3,4-dimethyl-5-isoxazolyl) benzenesulfonamide led to the identification of the biphenylsulfonamides as a novel series of endothelin-A (ETA) selective antagonists. Appropriate substitutions on the pendant phenyl ring led to improved binding as well as functional activity. A hydrophobic group such as isobutyl or isopropoxyl was found to be optimal at the 4'-position. Introduction of an amino group at the 2'-position also led to improved analogues. Combination of the optimal 4'- isobutyl substituent with the 2'-amino function afforded an analogue (20, BMS-187308) with improved ET(A) binding affinity and functional activity. Compound 20 also has good oral activity in inhibiting the pressor effect caused by an ET-1 infusion in rats. Doses of 10 and 30 μmol/kg iv 20 attenuated the pressor responses due to the administration of exogenous ET-1 to conscious monkeys, indicating that the compound inhibits the in vivo activity of endothelin-1 in nonhuman primates.
PHENYL SULFONAMIDE ENDOTHELIN ANTAGONISTS
-
, (2008/06/13)
Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R 1, R 2 and R. sup.3 are each independently(a) hydrogen, except that R. sup.1 is other than hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z 1, Z 2 and Z. sup.3 ;(c) halo;(d) hydroxyl;(e) cyano; (f) nitro; (g)--C(O)H or--C(O)R 6 ;(h)--CO 2 H or--CO 2 R 6 ; (i)--SH,--S(O) n R 6,--S(O) m--OH,--S(O) m--OR 6,--O--S(O) m--R 6,--O--S(O) m OH or--O--S(O) m--OR. sup.6 ;(j)--Z. sup.4--NR 7 R 8 ; or (k)--Z 4--N(R 11--Z 5--NR 9 R 10 ; and the remaining symbols are as defined in the specification.
INDOLE DERIVATIVES AND THEIR USE FOR TESTOSTERONE 5-ALPHA-REDUCTASE-MEDIATED DISEASES
-
, (2008/06/13)
Indole derivatives of the formula and pharmaceutical compositions thereof. They are useful for treating or preventing testosterone 5-alpha-reductase-mediated diseases, such as alopecia, acnes and prostatism
Nucleophilic Substitution Reactions in m-Nitrobenzylic Substrates
Barker, Steven D.,Norris, Robert K.
, p. 81 - 95 (2007/10/02)
The reaction of m-nitrobenzyl 2,4,6-trimethylbenzoate (11) with the salt (2) of 2-nitropropane, or the thiolate (16), gives moderate yields of substitution products .However, the mechanism of formation of these products could not be defi
