- Synthesis of 4-oxazolinephenylboronic acid and heterobiaryl oxazolines via a Suzuki reaction
-
An efficient synthesis of 4-oxazolinephenylboronic acid from 4-bromobenzoic acid is reported. The title compound couples with heteroaryl halides in presence of Pd(PPh3)4 and Na2CO3 in aqueous toluene to give het
- Ghosh, Samir,Kumar, A.Sanjeev,Mehta,Soundararajan,Sen, Subhabrata
-
scheme or table
p. 205 - 207
(2009/11/30)
-
- NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND BENAMIDE COMPOUNDS AND DRUGS CONTAINING THE SAME
-
Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases. In formula (I), R1 and R2 represent alkyl, alkoxy, cycloalkyl, phenyl, alkenyl, alkynyl, or a five- or six-membered saturated or unsaturated heterocyclic ring, or R1 and R2, together with a nitrogen atom to which R1 and R2 are attached, may form a ring; R3 and R4 represent a hydrogen atom, alkyl, a halogen atom, hydroxyl, nitrile, alkoxycarbonyl, alkoxy, or carboxyl; or R2 and R3 may be attached to each other to form -(CH2)m-, -N=CH-, -CH=N-, or -(C1-6 alkyl)C=N-; A, D, E, and G each represent a carbon atom, or any one of A, D, E, and G represents a nitrogen atom with the other three each representing a carbon atom; Q represents a nitrogen atom or a carbon atom; Y represents a group represented by formula (II) wherein X represents a hydrogen atom, group -C(=O)N(R5)R6 or group -C(=O)OR7, R8 is absent or represents a bond, an oxygen atom, a sulfur atom, -SO2-, -SO-, -CH2-CH2-, or - CH=CH-, and R9 and R10 represent a hydrogen atom, alkyl, alkoxy, a halogen atom, or hydroxyl; and Z represents - (CH2)n-, -O-(CH2)i-, or -C(=O)NH-(CH2)i-.
- -
-
-
- Positional isomers and analogs of mazindol as potential inhibitors of the cocaine binding site on the dopamine transporter site
-
A series of compounds, where the keto-tautomeric form of mazindol (2b) was modified by placing the 2-(p-chlorobenzoyl) portion of the molecule in the 3- and 4-positions, substituting the imidazo ring A by a 4,4-dimethyl 1- 2-oxazolo ring, and replacing th
- Houlihan, William J.,Boja, John W.,Kopajtic, Theresa A.,Kuhar, Michael J.,Degrado, Sylvia J.,Toledo, Leonel
-
-
- Fluoride ion-induced cyclization of o-[bis(trimethylsilyl)methyl]-N-acylbenzamide derivatives. New efficient synthesis of 2,3-differentially substituted 1(2H)-isoquinolones
-
A wide variety of 2-alkyl-3-alkyl, -3-aryl and -3-heteroaryl-1(2H)-isoquinolones have been obtained by fluoride ion-induced intramolecular alkenation of o-[bis(trimethylsilyl)methyl]-N-acylbenzamide derivatives.
- Couture, Axel,Cornet, Helene,Deniau, Eric,Grandclaudon, Pierre,Lebrun, Stephane
-
p. 469 - 476
(2007/10/03)
-
- Rational Design and Synthesis of a Highly Effective Transition State Anolog Inhibitor of the RTEM-1 β-Lactamase
-
The synthesis of (1R)-1-acetamido-2-(3-carboxyphenyl)ethane boronic acid, a rationally designed transition state anolog competitive inhibitor of the RTEM-1 β-lactamase from Escherichia coli, is reported.Kinetic measurements show that, as designed, it is a
- Martin, Richard,Bryan Jones, J.
-
p. 8399 - 8402
(2007/10/02)
-
- Synthesis and biological activity of new 3-hydroxy-3-methylglutaryl-CoA synthase inhibitors: 3-Oxetanones with a side chain mimicking the extended structure of 1233A
-
Structural analogs of 1233A, a microbial metabolite inhibiting 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase, were designed and synthesized. The 2-oxetanone moiety was left intact. All analogs prepared were tested for inhibition of HMG-CoA synt
- Hashizume,Ito,Morikawa,Kanaya,Nagashima,Usui,Tomoda,Sunazuka,Kumagai,Omura
-
p. 2097 - 2107
(2007/10/02)
-