- Stereoselective synthesis of diazabicyclic β-lactams through intramolecular amination of unactivated C(sp3)-H bonds of carboxamides by palladium catalysis
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An efficient C(sp3)-H bond activation and intramolecular amination reaction via palladium catalysis at the β-position of carboxyamides to make β-lactams was described. The investigation of the substrate scope showed that the current reaction conditions favored activation of the β-methylene group. Short sequences were developed for preparation of various diazabicyclic β-lactam compounds with this method as the key step from chiral proline and piperidine derivatives.
- Zhang, Shi-Jin,Sun, Wen-Wu,Cao, Pei,Dong, Xiao-Ping,Liu, Ji-Kai,Wu, Bin
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p. 956 - 968
(2016/02/19)
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- Chemoselective synthesis of N-protected alkoxyprolines under specific solvation conditions
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N-Protected hydroxyprolines (Hyp) were transformed chemoselectively into alkoxyproline derivatives by direct O-alkylation. The starting Hyp was transformed into the corresponding dianion in a mixture of dimethyl sulfoxide and tetrahydrofuran (1:16 v/v) as solvent. Under these conditions, the carboxy-anion showed reduced nucleophilicity because it was specifically solvated, and the more reactive oxy-anion was selectively alkylated. N-Protected trans-4-alkoxy-, cis-4-alkoxy- and trans-3-alkoxyprolines were thus obtained in a single step in very high overall yields and with complete stability of the stereogenic center configuration. Copyright
- Mihali, Voichita,Foschi, Francesca,Penso, Michele,Pozzi, Gianluca
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supporting information
p. 5351 - 5355
(2014/10/15)
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- BI-1H-BENZIMIDAZOLES AS HEPATITIS C VIRUS INHIBITORS
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The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
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Page/Page column 121
(2010/04/03)
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- Tyrosine kinase inhibitors
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The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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- Synthesis and Pharmacological Activity of Angiotensin Converting Enzyme Inhibitors: N-(Mercaptoacyl)-4-substituted-(S)-prolines
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The synthesis of a series of N-(mercaptoacyl)-4-substituted-(S)-prolines (2 and 3) is described.These compounds were evaluated in vitro for inhibition of angiotensin-converting enzyme (ACE), and selected compounds were evaluated in vivo for ACE inhibition.The most potent compounds in vitro are 108, 109, 111, 114, and 116, having relative potencies of 1.0, 1.0, 1.3, 1.1, and 2.6 as compared to the potency of captopril.The most potent compounds in vivo intravenously are 108, 111, 114, 116, 117, and 97.
- Smith, Elisabeth M.,Swiss, Gerald F.,Neustadt, Bernard R.,Gold, Elijah H.,Sommer, Jane A.,et al.
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p. 875 - 885
(2007/10/02)
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