58287-77-7Relevant academic research and scientific papers
Synthesis of Vicinal Quaternary All-Carbon Centers via Acid-catalyzed Cycloisomerization of Neopentylic Epoxides
Schmid, Matthias,Sokol, Kevin R.,Wein, Lukas A.,Torres Venegas, Sofia,Meisenbichler, Christina,Wurst, Klaus,Podewitz, Maren,Magauer, Thomas
supporting information, p. 6526 - 6531 (2020/09/02)
We report our studies on the development of a catalytic cycloisomerization of 2,2-disubstituted neopentylic epoxides to produce highly substituted tetralins and chromanes. Termination of the sequence occurs via Friedel-Crafts-type alkylation of the remote (hetero)arene linker. The transformation is efficiently promoted by sulfuric acid and proceeds best in 1,1,1,3,3,3-hexafluoroisopropanol (HFIP) as the solvent. Variation of the substitution pattern provided detailed insights into the migration tendencies and revealed a competing disproportionation pathway of dihydronaphthalenes.
Clickable coupling of carboxylic acids and amines at room temperature mediated by SO2F2: A significant breakthrough for the construction of amides and peptide linkages
Wang, Shi-Meng,Zhao, Chuang,Zhang, Xu,Qin, Hua-Li
, p. 4087 - 4101 (2019/04/30)
The construction of amide bonds and peptide linkages is one of the most fundamental transformations in all life processes and organic synthesis. The synthesis of structurally ubiquitous amide motifs is essential in the assembly of numerous important molecules such as peptides, proteins, alkaloids, pharmaceutical agents, polymers, ligands and agrochemicals. A method of SO2F2-mediated direct clickable coupling of carboxylic acids with amines was developed for the synthesis of a broad scope of amides in a simple, mild, highly efficient, robust and practical manner (>110 examples, >90% yields in most cases). The direct click reactions of acids and amines on a gram scale are also demonstrated using an extremely easy work-up and purification process of washing with 1 M aqueous HCl to provide the desired amides in greater than 99% purity and excellent yields.
DELTA OPIOID AGONIST, MU OPIOID ANTAGONIST COMPOSITIONS AND METHODS FOR TREATING PARKINSON'S DISEASE
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Page/Page column 19; 20, (2017/11/04)
The present invention provides for compositions and methods for the treatment of Parkinson's disease comprising a compound of formula (i): or a pharmaceutically effective salt or ester thereof alone or in combination with L-DOPA to provide a synergistic e
OLIGOMER-DIARYLPIPERAZINE CONJUGATES
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Paragraph 0303, (2015/12/07)
The invention relates to (among other things) oligomer-diarylpiperazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated diarylpiperazine compounds.
Controlled and chemoselective reduction of secondary amides
Pelletier, Guillaume,Bechara, William S.,Charette, Andre B.
supporting information; experimental part, p. 12817 - 12819 (2010/11/05)
This communication describes a metal-free methodology involving an efficient and controlled reduction of secondary amides to imines, aldehydes, and amines in good to excellent yields under ambient pressure and temperature. The process includes a chemoselective activation of a secondary amide with triflic anhydride in the presence of 2-fluoropyridine. The electrophilic activated amide can then be reduced to the corresponding iminium using triethylsilane, a cheap, rather inert, and commercially available reagent. Imines can be isolated after a basic workup or readily transformed to the aldehydes following an acidic workup. The amine moiety can be accessed via a sequential reductive amination by the addition of silane and Hantzsch ester hydride in a one-pot reaction. Moreover, this reduction tolerates various functional groups that are usually reactive under reductive conditions and is very selective to secondary amides.
METHOD OF TREATING PARKINSON'S DISEASE WITH DIARYLMETHYLPIPERAZINE COMPOUNDS EXHIBITING DELTA RECEPTOR AGONIST ACTIVITY
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Page/Page column 16, (2010/11/26)
Compositions and methods for treatment of Parkinson's disease to reduce the negative side effects of the disease by administering a therapeutically effective diarylmethylpiperazine compound which exhibits delta opioid receptor agonist activity, and option
1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF
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Page/Page column 48, (2008/06/13)
Compounds of general formula (I) wherein D, E, R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
4(PHENYL-PIPERAZINYL-METHYL) BENZAMIDE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF PAIN OR GASTROINTESTINAL DISORDERS
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Page 27, (2010/02/07)
Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particula
4(PHENYL-PIPERAZINYL-METHYL) BENZAMIDE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF PAIN OR GASTROINTESTINAL DISORDERS
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Page 33, (2010/02/07)
Compounds of general formula (I) wherein R1, R2 and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in the
Novel compounds
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, (2008/06/13)
Compounds of general formula (I), wherein R1 is selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl; each phenyl ring and heteroaromatic ring optionally and independently being further substituted by 1, 2 or 3 substituents selected
