- A Gold-Catalyzed A3 Coupling/Cyclization/Elimination Sequence as Versatile Tool for the Synthesis of Furfuryl Alcohol Derivatives from Glyceraldehyde and Alkynes
-
The reaction of glyceraldehyde with alkynes delivers furfuryl alcohol derivatives within only one reaction step in the presence of a gold(III) catalyst. The reaction cascade is initiated by an intermolecular gold-catalyzed A3 coupling sequence in which mo
- Li, Jian,Rudolph, Matthias,Rominger, Frank,Xie, Jin,Hashmi., A. Stephen K.
-
-
Read Online
- Synthesis of 2,5-Diaryl Nonsymmetric Furans C6-Platform Chemicals via Catalytic Conversion of Biomass and the Formal Synthesis of Dantrolene
-
Biomass-derived commodity chemical 5-hydroxymethyl furfural is an underutilized C6-platform chemical derived from cellulose that is ideal to prepare next-generation value-added products. We have developed an efficient synthetic strategy to access 2,5-diar
- Chacón-Huete, Franklin,Lasso, Juan David,Szavay, Paul,Covone, Jason,Forgione, Pat
-
p. 515 - 524
(2020/12/22)
-
- Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors
-
In this present study, a series of 5-phenyl-2-furan and 4-phenyl-2-oxazole derivatives were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. In vitro results showed that the synthesized compounds exhibited considerable inhibitory ac
- Lin, Yinuo,Ahmed, Wasim,He, Min,Xiang, Xuwen,Tang, Riyuan,Cui, Zi-Ning
-
-
- URIDINE NUCLEOSIDE DERIVATIVES, COMPOSITIONS AND METHODS OF USE
-
This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to compounds, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.
- -
-
Paragraph 0191; 0198; 0243
(2018/04/20)
-
- PREMATURE-TERMINATION-CODONS READTHROUGH COMPOUNDS
-
Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.
- -
-
Page/Page column 0250; 0282; 0283
(2013/10/22)
-
- Efficient Pd-catalyzed direct arylations of heterocycles with unreactive and hindered aryl chlorides
-
A highly electron-rich Pd complex can efficiently catalyze the direct arylation of heteroaromatics with unreactive and sterically congested aryl chlorides.
- Ghosh, Debalina,Lee, Hon Man
-
supporting information
p. 5534 - 5537,4
(2012/12/12)
-
- 2-amino-3-(5-phenylfuran-2-yl)propionic acids and 5-phenylfuran-2-ylacrylic acids are novel substrates of phenylalanine ammonia-lyase
-
Both racemic 2-amino-3-(5-phenylfuran-2-yl)propionic acids and 5-phenylfuran-2-ylacrylic acids were synthesized and spectroscopically characterized (UV, EI-MS, 1H-NMR and 13C-NMR). The phenyl group of the 5-phenylfuranyl residue carried no (rac-la) para-Br (rac-lb) or Cl para or ortho (rac-lc, d) substituents. The novel furanylalanines were used as substrates of recombinant phenylalanine ammonia-lyase (PAL). When 50% of the racemic 5-phenylfuranylalanines were converted into the corresponding acrylates, the D-enantiomers of the substrates could be isolated. The L-enantiomers could be prepared from the substituted acrylates when the PAL reaction was reversed in the presence of 6 M ammonia at pH 10. The Japan Institute of Heterocyclic Chemistry.
- Paizs, Csaba,Tosa, Monica Ioana,Bencze, Laszlo Csaba,Brem, Juergen,Irimie, Florin Dan,Retey, Janos
-
experimental part
p. 1217 - 1228
(2011/05/05)
-
- Synthesis and evaluation of compounds that induce readthrough of premature termination codons
-
A structure-activity relationship (SAR) study was carried out to identify novel, small molecular weight compounds which induce readthrough of premature termination codons. In particular, analogs of RTC13, 1, were evaluated. In addition, hypothesizing that these compounds exhibit their activity by binding to the ribosome, we prepared the hybrid analogs 13 containing pyrimidine bases and these also showed good readthrough activity.
- Jung, Michael E.,Ku, Jin-Mo,Du, Liutao,Hu, Hailiang,Gatti, Richard A.
-
supporting information; experimental part
p. 5842 - 5848
(2011/10/18)
-
- Intramolecular reactions of alkynes with furans and electron rich arenes catalyzed by PtCl2: The role of platinum carbenes as intermediates
-
5-(2-Furyl)-1-alkynes react, with PtCl2 as catalyst, to give phenols. On the basis of DFT calculations, a cyclopropyl platinacarbene complex was found as the key intermediate in the process. The cyclopropane and dihydrofuran rings of this intermediate open to form a carbonyl compound, which reacts with the platinum carbene to form an oxepin, which is in equilibrium with an arene oxide. When the reaction is carried out in the presence of water, dicarbonyl compounds are obtained, which support the proposed mechanism. Other cyclizations of alkynes with furans or electron-rich arenes give products of apparent Friedel-Crafts-type reactions, although these processes could also proceed by pathways involving the formation of cyclopropyl platinum carbenes.
- Martin-Matute, Belen,Nevado, Cristina,Cardenas, Diego J.,Echavarren, Antonio M.
-
p. 5757 - 5766
(2007/10/03)
-
- Inhibitors of protein isoprenyl transferases
-
Compounds having the formula STR1or a pharmaceutically acceptable salt thereof wherein R 1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L 2 --, and (i) heterocyclic-L 2 --; R 2 is selected from STR2(b) --C(O)NH--CH(R 14)--C(O)OR 15, STR3(d) --C(O)NH--CH(R 14)--C(O)NHSO 2 R 16, (e) --C(O)NH--CH(R 14)-tetrazolyl, (f) --C(O)NH-heterocyclic, and (g) --C(O)NH--CH(R 14)--C(O)NR 17 R 18 ; R 3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R 4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L 1 is absent or is selected from (a) --L 4 --N(R 5)--L 5 --, (b) --L 4 --O--L 5 --, (c) --L 4 --S(O) n --L 5 -- (d) --L 4 --L 6 --C(W)--N(R 5)--L 5 --, (e) --L 4 --L 6 --S(O)m--N(R 5)--L 5 --, (f) --L 4 --N(R 5)--C(W)--L 7 --L 5 --, (g) --L 4 --N(R 5)--S(O) p --L 7 --L 5 --, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
- -
-
-
- Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase
-
Potent and orally bioavailable nonthiol-containing inhibitors of protein farnesyltransferase are described. Oral bioavailability was achieved by replacement of the pyridyl ether moiety of 1 with a 2-substituted furan ether to give 4. Potency was regained with 2,5-disubstituted furan ethers while maintaining the bioavailability inherent in 4. p-Chlorophenylfuran ether 24 is 0.7 nM in vitro (FTase) and is 32% bioavailable in the mouse, 30% bioavailable in rats, and 21% bioavailable in dogs.
- Augeri, David J.,Janowick, Dave,Kalvin, Douglas,Sullivan, Gerry,Larsen, John,Dickman, Daniel,Ding, Hong,Cohen, Jerry,Lee, Jang,Warner, Robert,Kovar, Peter,Cherian, Sajeev,Saeed, Badr,Zhang, Haichao,Tahir, Steve,Ng, Shi-Chung,Sham, Hing,Rosenberg, Saul H.
-
p. 1069 - 1074
(2007/10/03)
-