119740-95-3Relevant academic research and scientific papers
FLUOROMETHYL-SUBSTITUTED PYRROLE CARBOXAMIDES
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Paragraph 0780, (2014/03/25)
The invention relates to pyrrole carboxamides bearing a fluoromethyl-moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
FLUOROMETHYL-SUBSTITUTED PYRROLE CARBOXAMIDES
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Page/Page column 157; 158, (2014/03/25)
The invention relates to pyrrole carboxamides bearing a fluoromethyl- moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Constructions of tetrahydro-γ-carboline skeletons via intramolecular oxidative carbon-carbon bond formation of enamines
Lv, Jinglei,Li, Ji,Zhang-Negrerie, Daisy,Shang, Siyun,Gao, Qingzhi,Du, Yunfei,Zhao, Kang
supporting information, p. 1929 - 1932 (2013/06/04)
The synthetically and biologically important 4-methyl and 4-methoxy tetrahydro-γ-carboline compounds were readily synthesized in high yields from an aryl amine and a 5-amino-3-oxopentanoate derivative through a series of reactions of enamination, oxidative annulation, deprotection/lactamization and the final reduction reaction of the carbonyl group. The underpinning strategy involves the oxidative C(sp2)-C(sp2) bond formation realized by either Pd(OAc)2/Cu(OAc)2 or a hypervalent iodine reagent.
1,3,4-OXADIAZOLE AND 1,3,4-THIADIAZOLE BETA-LACTAMASE INHIBITORS
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Page/Page column 87; 88, (2013/10/21)
β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
Dibutylphosphate (DBP) mediated synthesis of cyclic N,N′- disubstituted urea derivatives from amino esters: A comparative study
Agrawal, Sumit K.,Sathe, Manisha,Kaushik, M. P.,Halve, A. K.
, p. 5996 - 5999,4 (2020/08/20)
The N,N′-disubstituted urea derivatives such as amino acid hydantoins and dihydrouracil derivatives were prepared starting from natural and unnatural amino acid esters using dibutylphosphate (DBP). During the attempted synthesis of N-heterocycles with larger than six-membered rings containing the N,N′-disubstituted urea functionalities, three unexpected products namely squamolone, N-methyl pyrrolidine-2-one, and diketopiperazine were isolated.
New approaches for the synthesis of isotopically labelled guanidine-derived amino acids and noradrenaline reuptake inhibitors
Bischoff, Roland,Hamilton, Deborah J.,Jobson, Nicola K.,Sutherland, Andrew
, p. 323 - 326 (2008/02/05)
A new approach for the stereoselective synthesis of guanidine-derived amino acids, L-arginine and (+)-blastidic acid, has been devised which allows the selective incorporation of isotopic labels in both the side chain of the amino acid as well as the guanidine unit. A new asymmetric synthesis of the (S,R)-diastereomer of reboxetine, an antidepressant, has also been completed which allows the specific incorporation of radiolabelled iodine for SPECT imaging. Copyright
A highly efficient, asymmetric synthesis of blastidic acid: The β-amino acid component of the antibiotic, (+)-blasticidin S
Bischoff, Roland,McDonald, Niall,Sutherland, Andrew
, p. 7147 - 7149 (2007/10/03)
A new approach for the asymmetric synthesis of blastidic acid, the β-amino acid component of the antibiotic, (+)-blasticidin S has been achieved in 11 steps and 30% overall yield. The key transformations involve a one-pot Swern/Wittig reaction sequence to
Synthesis and antinociceptive activity of orally active opioid peptides: Improvement of oral bioavailability by esterification
Ogawa, Tadashi,Araki, Mamoru,Miyamae, Tetsuhisa,Okayama, Toru,Hagiwara, Masaki,Sakurada, Shinobu,Morikawa, Tadanori
, p. 759 - 771 (2007/10/03)
To improve the oral bioavailability of a dermorphin tetrapeptide analog, Nα-1-iminoethyl-Tyr-D-MetO-Phe-MeβAla-OH (III), 1) which has a potent analgesic activity after oral administration, various derivatives were synthesized to incr
Tandem radical cyclisations: Synthesis of lysergic acid derivatives
Ozlu,Cladingboel,Parsons
, p. 2183 - 2206 (2007/10/02)
A novel free radical cyclisation approach for the synthesis of lysergic acid analogues has been investigated. The homolytic cleavage of carbon- bromine bond, mediated by tri-n-butyltin hydride, led to the development of a method for the construction of 3,
New Histidyl amino acid derivatives, and pharmaceutical composition comprising the same
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, (2008/06/13)
A compound of the formula: STR1 wherein R1 is lower alkyl optionally substituted with a substituent selected from the group consisting of acyl, hydroxy, lower alkoxy, aryl, lower alkylthio and a group of the formula: STR2 in which R5 is hydrogen or acyl and R6 is hydrogen or lower alkyl; aryl; or amino optionally substituted with substituent(s) selected from the group consisting of lower alkyl and acyl; and R2 is hydrogen or lower alkyl; or R1 and R2 are taken together with the attached nitrogen atom to form a heterocyclic group optionally substituted with substituent(s) selected from the group consisting of lower alkyl, hydroxy(lower )alkyl, lower alkoxy(lower)alkyl, acyl(lower)alkyl, oxo and acyl; R3 is hydrogen or lower alkyl; and R4 is lower alkyl; and its pharmaceutically acceptable salt, processes for the preparation thereof and pharmaceutical composition comprising the same.
