25040-17-9Relevant academic research and scientific papers
Facile and simple synthesis of N -alkyl and N -aryl 2-benzazepines by nucleophilic heteroannulation
Srinivasan,Rajashekar,Shyamapada,Syam Kumar
supporting information, p. 3112 - 3121 (2015/10/12)
An efficient and practical synthesis of N-alkyl and N-aryl 2-benzazepine has been developed. The key steps involved in the synthesis were palladium-mediated Heck reaction followed by aza heterocyclic ring construction by nucleophilic heteroannulation. This four-step sequence synthetic protocol gave moderate to good yields for a wide range of substrates. Subsequently, functionalization of the synthesized compound was carried out under Heck and Suzuki reaction conditions.
Synthesis and antifungal activity of 7-methyl-7-hydroxy-2,3-benzo[c]octa-1, 6-olide
Zhao, Jin,Dong, Hong-Bo,Yang, Ming-Yan,Du, Juan,Jiang, Jia-Zheng,Wang, Ming-An
, p. 312 - 317 (2014/02/14)
The racemic 7-methyl-7-hydroxy-2,3-benzo[c]octa-1,6-olide, the analog of natural product (6R)-3,7-dimethyl-7-hydroxy-2-octen-1,6-olide, was totally synthesized using easily available (E)-2-(2-carboxyvinyl)benzoic acid as a raw material in nine-step reacti
Solvent effect in reactions using strykers reagent
Sass, Daiane Cristina,Heleno, Vladimir Constantino Gomes,Cavalcante, Simone,Da Silva Barbosa, Jader,Soares, Ana Carolina Ferreira,Constantino, Mauricio Gomes
, p. 9374 - 9378 (2013/01/15)
The solvent has a significant influence in the rate of reactions promoted by Strykers reagent. The reactions performed in THF were, in most cases, faster than in toluene.
Nitroxyl radical/PhI(OAc)2: One-pot oxidative cleavage of vicinal diols to (di)carboxylic acids
Shibuya, Masatoshi,Shibuta, Takuro,Fukuda, Hayato,Iwabuchi, Yoshiharu
, p. 5010 - 5013 (2013/01/15)
A mild and user-friendly one-pot oxidative cleavage of vicinal diols to their corresponding (di)carboxylic acids using AZADOs and PhI(OAc)2 is described. 1,2-Diols and 2,3-diols as well as 1,2,3-triol gave one- or two-carbon-unit-shorter carboxylic acids. Internal vicinal diols also smoothly underwent one-pot oxidative cleavage to afford the corresponding dicarboxylic acids. Cyclic vicinal diols are converted to their corresponding open-form dicarboxylic acids.
New synthetic methodology for construction of the 3,4-dihydroisoquinolinone skeleton: A key structure for isoquinoline alkaloids
Muejde, Berk,Oezcan, Sevil,Balci, Metin
, p. 407 - 410 (2012/04/10)
We hereby report a new method for preparation of 3,4-dihydroisoquinolin- 1(2H)-one as well as isoquinolin-1(2H)-one skeleton starting from the methyl 2-(3-methoxy-3-oxopropyl)benzoate. The ester functionality, adjacent to the methylene, was regiospecifically converted to the desired acyl azide. The isocyanate was transformed into the monoisocyanate by Curtius rearrangement followed by trapping with aniline. The formed urea derivative was cyclized with NaH to give a 3,4-dihydroisoquinolin-1(2H)-one derivative. Incorporation of a double bond into the six-membered ring followed by removal of the substituent resulted in the formation of isoquinolin-1(2H)-one skeleton.
N- INDEN- 2 -YL- ISOPROPYLSULFONAMIDES AS AMPA RECEPTOR POTENTIATORS
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Page/Page column 22-23, (2010/07/10)
A compound of formula (I) and salts thereof are provided: Wherein n and R1 are defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or
Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan
Kamei, Katsuhide,Maeda, Noriko,Nomura, Kayoko,Shibata, Makoto,Katsuragi-Ogino, Ryoko,Koyama, Makoto,Nakajima, Mika,Inoue, Teruyoshi,Ohno, Tomochika,Tatsuoka, Toshio
, p. 1978 - 1992 (2007/10/03)
A new series of 1,4-benzoxazepine derivatives was designed, synthesized, and evaluated for binding to 5-HT1A receptor and cerebral anti-ischemic effect. A lot of compounds exhibited nanomolar affinity for 5-HT1A receptor with good selectivity over both dopamine D 2 and α1-adrenergic receptors. Among these compounds, 3-chloro-4-[4-[4-(2-pyridinyl)-1,2,3,6-tetrahydropyridin-1-yl]butyl]- 1, 4-benzoxazepin-5(4H)-one (50: SUN N4057 (Piclozotan) as 2HCl salt) showed remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model.
A simple method for the preparation of monomethyl esters of dicarboxylic acids by selective esterification of the nonconjugated carboxyl group in the presence of an aromatic or conjugated carboxyl group
Ram, Ram N.,Meher, Nabin Kumar
, p. 282 - 283 (2007/10/03)
Various dicarboxylic acids have been converted selectively into monomethyl esters in which the nonconjugated carboxyl group is selectively esterified in the presence of an aromatic or conjugated carboxyl group at room temperature (~ 25-27°C) in methanol using a catalytic amount of thionyl chloride.
α-nitrocycloalkanones as a source of α,ω,-dicarboxylic acid dimethyl esters
Ballini, Roberto,Bosica, Giovanna
, p. 16131 - 16138 (2007/10/03)
α,ω-Dicarboxylic acid dimethyl esters arc easily obtained by ring cleavage of α-nitrocycloalkanones. Thus, reaction of the latter compounds with three equivalents of potassium persulfate, in methanol and in presence of sulfuric acid at 80 °C, provides α,ω-dicarboxylic acid dimethyl esters in high yields. Long-chain, and alkylated α,ω-dicarboxylic acid dimethyl esters can be also efficiently obtained.
Fused 7-membered cyclic compound and antipsychotic preparation containing the same
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, (2008/06/13)
A fused cyclic compound having the formula (I) or salts thereof: ψψ ψwherein both of A and B are carbonyl groups, or one represents methylene group and the other carbonyl group, Z represents a sulfur atom, or a nitrogen atom which may be substituted, or a methylene group, R represents an aromatic or heterocyclic group, which may be substituted, X represents a hydrogen atom, a halogen atom, a C1 - C5 lower alkyl group, a C1 - C5 lower alkoxy group, a C7 - C9 arylalkoxy group, a C1 - C5 lower acyloxy group, a C7 - C10 arylcarbonyloxy group, a hydroxy group, a nitro group or an ester group, and n is an integer of 2 to 10. The compounds have affinity for serotonin receptor.ψ
