76348-92-0Relevant articles and documents
Molecular Oxygen-Mediated Minisci-Type Radical Alkylation of Heteroarenes with Boronic Acids
Zhang, Lizhi,Liu, Zhong-Quan
, p. 6594 - 6597 (2017/12/26)
The carbon-carbon bond formation via autoxidation of organoboronic acid using 1 atm of O2 is achieved in a simple, clean, and green fashion. The approach allows a technically facile and environmentally benign access to structurally diverse heteroaromatics with medicinally privileged scaffolds. The strategy also displays its practicality and sustainability in the resynthesis of marketed drugs Crestor and pyrimethamine.
CYCLIC AMINE COMPOUND AND USE THEREOF
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Page/Page column 163-164; 165-166; 166-167, (2010/11/28)
The present invention relates to a compound represented by the formula:( I ) wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent (s); U, V and W are each independently C or N, provided that when any one of U, V and W is N, then the others should be C; Ra and Rb are each independently a cyclic group optionally having substituent (s), a C1-10 alkyl group optionally having substituent (s), a C2-10 alkenyl group optionally having substituent (s), or a C2-10alkynyl group optionally having substituent (s); X is a bond, or a spacer having 1 to 6 atoms in the main chain; Y is a spacer having 1 to 6 atoms in the main chain; Rc is a hydrocarbon group optionally containing heteroatom(s) as the constituting atom(s), which optionally has substituent (s); m and n are each independently 1 or 2; and ring B optionally further has substituent (s), or a salt thereof. The compound of the present invention has excellent renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension, and the like.
Lipid-Lowering Effects of Ethyl 2-Phenacyl-3-aryl-1H-pyrrole-4-carboxylates in Rodents
Holub, Justin M.,O'Toole-Colin, Kathy,Getzel, Adam,Argenti, Anthony,Evans, Michael A.,Smith, Daniel C.,Dalglish, Gerard A.,Rifat, Shahzad,Wilson, Donna L.,Taylor, Brett M.,Miott, Ulander,et al.
, p. 135 - 157 (2007/10/03)
A series of substituted 2-phenacyl-3-phenyl-1H-pyrrole-4-carboxylates were prepared from substituted acetophenones in 6 steps. The final condensations between a chloroenal and an aminoketone were carried out under neutral conditions in parallel to yield the series listed below. Selected pyrrole derivatives proved to be potent hypolipidemic agents lowering serum triglyceride concentrations in CF-1 male mice after 14 days of I.P. administration. One agent orally lowered serum cholesterol in Sprague-Dawley male rats at 2 mg/kg/day after 14 days. The agents demonstrated a lowering of mouse serum LDL-cholesterol levels and selected compounds showed an elevation of serum HDL-cholesterol levels. The cholesterol concentrations in the liver were raised while the cholesterol and triglyceride contents of the aorta were significantly lowered by the selected trisubstituted pyrrole.
AGENT FOR PREVENTING OR TREATING NEUROPATHY
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Page/Page column 111-112; 114, (2010/02/06)
The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula:wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s);B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group;X is a divalent acyclic hydrocarbon group;Z is -O-, -S-, -NR2-, -CONR2- or -NR2CO- (R2 is a hydrogen atom or an optionally substituted alkyl group);Y is a bond or a divalent acyclic hydrocarbon group;R1 is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be -O-, or a salt thereof.
4-Substituted 1,5-diarylpyrazole, analogues of celecoxib: Synthesis and preliminary evaluation of biological properties
Menozzi, Giulia,Merello, Luisa,Fossa, Paola,Mosti, Luisa,Piana, Antonietta,Mattioli, Francesca
, p. 795 - 808 (2007/10/03)
A number of 5-aryl-1-[4-(methylsulfonyl)-phenyl]-1H-pyrazoles and 4-(5-aryl-1H-pyrazol-1-yl)benzenesulfonamides 3, 4, 5, 6, analogues of the COX-2 selective inhibitor celecoxib (celebrex), were synthesized. In order to verify the effects on the biological properties of certain substituents put on position 4 of the pyrazole nucleus, some of these compounds were screened in vivo for their anti-inflammatory and analgesic activities. Moreover, sodium salts of carboxylic acids 4 were tested in vitro for their platelet anti-aggregating properties. The results of these preliminary biological assays showed that new derivatives are not endowed with improved anti-inflammatory and analgesic properties, in comparison with celecoxib. In addition, docking studies were carried out on the most significative compounds to evaluate their interaction mode at the active site of both COX-1 and COX-2. Some remarks about the SAR of this class of COX-inhibitors are drown out.
An Improved General Synthesis of 4-Aryl-5-pyrimidinecarboxylates
Breaux, Eves J.,Zwikelmaier, Kurt E.
, p. 183 - 184 (2007/10/02)
We wish to report an improved, general synthesis of 4-aryl-5-pyrimidinecarboxylates 1.Two different routes have previously been reported for the synthesis of examples of this class of pyrimidine carboxylates.The parent compound, ethyl 4-phenyl-5-pyrimidinecarboxylate was prepared in low yield by the reaction of s-triazine with ethyl benzoyl acetate.In addition, the enol ether β-ketoaldehyde synthon, ethyl 2-benzoyl-3-ethoxy-2-propenoate, was reported to give 1a in modest yield when reacted with guanidine (2).
