M72803

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Showing 1-12 of 12 results for "M72803" within Papers

Acetoacetanilides as masked isocyanates: facile and efficient synthesis of unsymmetrically substituted ureas.

Ying Wei et al.

Organic letters, 12(19), 4220-4223 (2010-09-03)

A general and practical method for the preparation of unsymmetrically substituted ureas has been developed. By the reactions of acetoacetanilides with various amines including primary/secondary amines, a series of substituted aryl ureas were achieved in high yields. Acetoacetanilide substrates can

Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists.

Dmitry Zuev et al.

Bioorganic & medicinal chemistry letters, 20(12), 3669-3674 (2010-05-18)

A novel series of [6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethyl]-dialkylamines was discovered as potent CRF(1)R antagonists. The optimization of binding affinity in the series by the parallel reaction approach is discussed herein.

C-2 arylation of piperidines through directed transition-metal-catalyzed sp3 C-H activation.

Hana Prokopcová et al.

Chemistry (Weinheim an der Bergstrasse, Germany), 16(44), 13063-13067 (2010-10-29)

Efficient solid-phase synthesis of sulfotyrosine peptides using a sulfate protecting-group strategy.

Ahmed M Ali et al.

Angewandte Chemie (International ed. in English), 48(11), 2024-2026 (2009-02-05)

Double protection: Efficient Fmoc-based solid-phase synthesis (SPPS) of sulfotyrosine (sY) peptides is achieved by incorporating the sY residue(s) as a dichlorovinyl-protected (DCV) sulfodiester(s) and using 2-methylpiperidine for Fmoc removal. After removal of the other protecting groups, the DCV group could

Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity.

Xiaoqing Wu et al.

Bioorganic & medicinal chemistry, 18(11), 3812-3822 (2010-05-15)

There is an urgent need to design and develop new and more potent EGFR inhibitors with improved anti-tumor activity. Here we describe the design and synthesis of two series of 4-benzothienyl amino quinazolines as new analogues of the EGFR inhibitor

Synthesis of 2-aminobenzoxazoles using tetramethyl orthocarbonate or 1,1-dichlorodiphenoxymethane.

Christopher L Cioffi et al.

The Journal of organic chemistry, 75(22), 7942-7945 (2010-10-27)

The synthesis of 2-aminobenzoxazoles can be readily achieved by two versatile, one-pot procedures utilizing commercially available tetramethyl orthocarbonate or 1,1-dichlorodiphenoxymethane, an amine, and an optionally substituted 2-aminophenol. The reactions were conducted under mild conditions and provided 2-aminobenzoxazoles in modest to

Analysis of vibrational spectra of 2 and 3-methylpiperidine based on density functional theory calculations.

Yusuf Erdogdu et al.

Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 74(1), 162-167 (2009-07-04)

The experimental and theoretical vibrational spectra of 2 and 3-methylpiperidine (abbreviated as 2-MP and 3-MP) were studied. The FT-Infrared spectra of 2-MP and 3-MP molecules were recorded in the liquid phase. The structural and spectroscopic analysis of the title molecules

Structure-activity relationships of some pyridine, piperidine, and pyrrolidine analogues for enhancing and inhibiting the binding of (+/-)-[3H]nicotine to the rat brain P2 preparation.

J W Sloan et al.

Journal of medicinal chemistry, 28(9), 1245-1251 (1985-09-01)

Previous studies have shown that (+/-)-[3H]nicotine binds to multiple sites in the rat brain P2 preparation. Using a series of pyridine, piperidine and pyrrolidine analogues, the present studies identified drugs with specificity for a separate up-regulatory site that increases the

Fourth ventricle effects of nicotine, 2-methylpiperidine and cytisine in dogs.

W R Martin et al.

Pharmacology, biochemistry, and behavior, 25(4), 843-848 (1986-10-01)

Four distinguishable nicotinic binding sites have been identified as well as four nicotinic ligands with different specificities: (+/-)-2-methylpiperidine which binds to a very high affinity site (Site 1) and produces up-regulation of the high affinity site (Site 2); (-)-nicotine which

Opioid and nicotinic medullary hyperalgesic influences in the decerebrated rat.

W R Martin et al.

Pharmacology, biochemistry, and behavior, 29(4), 725-731 (1988-04-01)

The effects of ethylketazocine (EKC) administered intraperitoneally and the nicotinic ligands (-)- and (+)-nicotine, (-)-cytisine, (-)-lobeline, and (+)-2-methylpiperidine administered into the 4th ventricle on the latency of the thermally evoked withdrawal reflex of the decerebrate rat were investigated. EKC administered

Stereospecificity of 2-methylpiperidine binding to a nicotinic up-regulatory site in the rat brain P2 preparation.

J W Sloan et al.

Life sciences, 37(15), 1367-1372 (1985-10-14)

(+/-)-2-Methylpiperidine has a high degree of specificity in enhancing the binding of (-)-[3H]nicotine in the rat brain P2 preparation. (-)- and (+)-2-Methylpiperidine have been resolved. The (+) but not the (-) isomer increased the binding of (-)-[3H]nicotine. The two isomers

Gold-catalyzed efficient synthesis of azepan-4-ones via a two-step [5 + 2] annulation.

Li Cui et al.

Chemical communications (Cambridge, England), 46(19), 3351-3353 (2010-05-06)

A surprisingly efficient synthesis of azepan-4-ones via a two-step [5 + 2] annulation is developed. This reaction involves a key gold catalysis and shows generally high regioselectivities and good to excellent diastereoselectivities.

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