71998-69-1Relevant articles and documents
A convenient synthesis of the enantiomerically pure (S)-2,4-dihydroxybutyl-4-hydroxybenzoate using hydrolytic kinetic resolution
More, Namita A.,Jadhao, Nitin L.,Garud, Dinesh R.,Gajbhiye, Jayant M.
supporting information, p. 2093 - 2098 (2018/07/15)
(S)-2,4-Dihydroxybutyl-4-hydroxybenzoate was prepared in an extremely simple and practical way with high enantiomeric excess (99% ee) using Jacobsen’s Hydrolytic Kinetic Resolution technique as a key step and source of chirality.
SILVESTROL ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
-
, (2018/01/15)
The invention relates generally to a silvestrol molecule activated with a leaving group. The invention further relates generally to an antibody-drug conjugate comprising an antibody conjugated by a linker to one or more silvestrol drug moieties and methods of treatment.
Intramolecular thermal stepwise [2 + 2] cycloadditions: Investigation of a stereoselective synthesis of [n.2.0]-bicyclolactones
Throup, Adam,Patterson, Laurence H.,Sheldrake, Helen M.
supporting information, p. 9554 - 9559 (2016/10/22)
Fused cyclobutanes are found in a range of natural products and formation of these motifs in a straightforward and easy manner represents an interesting synthetic challenge. To this end we investigated an intramolecular variant of the thermal enamine [2 + 2] cyclisation, developing a diastereoselective intramolecular enamine [2 + 2] cyclisation furnishing δ lactone and lactam fused cyclobutenes in good yield and excellent diastereoselectivity.
Carbohydrate-Catalyzed Enantioselective Alkene Diboration: Enhanced Reactivity of 1,2-Bonded Diboron Complexes
Fang, Lichao,Yan, Lu,Haeffner, Fredrik,Morken, James P.
supporting information, p. 2508 - 2511 (2016/03/12)
Catalytic enantioselective diboration of alkenes is accomplished with readily available carbohydrate-derived catalysts. Mechanistic experiments suggest the intermediacy of 1,2-bonded diboronates.
Synthesis of Novel C-Pivot Lariat 18-Crown-6 Ethers and Their Efficient Purification
Jana, Susovan,Suresh, Vallabh,Lepore, Salvatore D.
, p. 1977 - 1980 (2015/09/01)
The syntheses of various lariat ethers including several not previously reported and their efficient purification are presented. The synthesis route brings together reactions from a variety of previous works leading to a robust and generalized approach to these C-pivot lariats. The main steps are condensation of functionalized diols with pentaethylene glycol ditosylate in the presence of potassium as a templating cation. Purification of the final products was achieved without chromatography by extracting from an aqueous potassium hydroxide solution.
A concise stereoselective total synthesis of diplodialide C
Pratapareddy, Bommareddy,Sreenivasulu, Reddymasu,Hatti, Islavathu,Venkata Basaveswara Rao, Mandava,Raju, Rudraraju Ramesh
, p. 1921 - 1926 (2015/10/29)
An asymmetric total synthesis of diplodialide C has been achieved starting from commercially available homoallylic alcohol. Regioselective opening of the chiral epoxide, cross-metathesis reaction, and Yamaguchi macrolactonization were used as the key step
Asymmetric Oxy-Michael Addition to γ-Hydroxy-α,β-Unsaturated Carbonyls Using Formaldehyde as an Oxygen-Centered Nucleophile
Yoneda, Naoki,Hotta, Ayano,Asano, Keisuke,Matsubara, Seijiro
, p. 6264 - 6266 (2015/02/19)
Formaldehyde was utilized as an oxygen-centered nucleophile in an asymmetric oxy-Michael addition to γ-hydroxy-α,β-unsaturated carbonyl compounds using bifunctional organocatalysts through hemiacetal intermediates. The cyclic acetal product could be further transformed into β-hydroxycarbonyl compounds, useful synthetic intermediates leading to various important target molecules. As such, this method is an example of a novel formal asymmetric hydration of α,β-unsaturated carbonyl compounds.
A new enantioselective synthesis of the anticonvulsant drug pregabalin (lyrica) based on a hydrolytic kinetic resolution method
Mujahid, Mohammad,Muthukrishnan, Murugan
, p. 965 - 969 (2014/01/06)
A practical and efficient enantioselective synthesis of the anticonvulsant drug pregabalin is described for the first time using Jacobsen's hydrolytic kinetic resolution of a terminal epoxide as a key step and a source of chirality.
MATRIX METALLOPROTEINASE INHIBITORS
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, (2012/04/10)
The present invention relates to methyl sulfonamides and N-formamides derivatives of formula (I) and to processes for their syntheses. The invention also relates to pharmacological compositions containing these derivatives and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatie arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, dry eye, neointimal proliferation which leads to restenosis and ischemic heart failure, stroke, renal disease, tumor metastasis, and other inflammatory disorders characterized by over expression and over activation of an matrix metalloproteinase using the compounds.
Lewis acid-promoted addition of 1,3-bis(silyl)propenes to aldehydes: A route to 1,3-dienes
Borg, Tessie,Tuzina, Pavel,Somfai, Peter
experimental part, p. 8070 - 8075 (2011/11/28)
The Lewis acid-promoted addition of 1,3-bis(silyl)-propenes to aldehydes to provide the corresponding (E)-1,3-dienes in excellent stereoselectivity and good to excellent yields is reported. The procedure is mild, base-free, and operationally straightforward.
