- Rapid and efficient synthesis of 1-Arylpiperazines under microwave irradiation
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1-Arylpiperazines, finding wide applicability in pharmaceuticals were synthesized easily under microwave irradiation from bis(2-chloroethyl)amine hydrochloride and substituted anilines without any solvent. The reaction time was just 1-3 mins. 1-Arylpiperazines were synthesized in 53 to 73% yields. Potent serotonin ligands like Trifluoromethylphenylpiperazine (TFMPP) and 3-Chlorophenylpiperazine (mCPP) were also prepared in just 1 min and 2 mins respectively.
- Jaisinghani, Harsha G.,Khadilkar, Bhushan M.
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Read Online
- Identification of novel GLUT inhibitors
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The compound class of 1H-pyrazolo[3,4-d]pyrimidines was identified using HTS as very potent inhibitors of facilitated glucose transporter 1 (GLUT1). Extensive structure–activity relationship studies (SAR) of each ring system of the molecular framework was established revealing essential structural motives (i.e., ortho-methoxy substituted benzene, piperazine and pyrimidine). The selectivity against GLUT2 was excellent and initial in vitro and in vivo pharmacokinetic (PK) studies are encouraging.
- Siebeneicher, Holger,Bauser, Marcus,Buchmann, Bernd,Heisler, Iring,Müller, Thomas,Neuhaus, Roland,Rehwinkel, Hartmut,Telser, Joachim,Zorn, Ludwig
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p. 1732 - 1737
(2016/07/27)
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- Pd-Catalyzed Synthesis of Piperazine Scaffolds under Aerobic and Solvent-Free Conditions
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A facile Pd-catalyzed methodology providing an efficient synthetic route to biologically relevant arylpiperazines under aerobic conditions is reported. Electron donating and sterically hindered aryl chlorides were aminated to afford yields up to 97%, with examples using piperazine as solvent, illustrating an ecofriendly, cost-effective synthesis of these privileged structures.
- Reilly, Sean W.,Mach, Robert H.
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supporting information
p. 5272 - 5275
(2016/10/31)
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- INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
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The present invention provides novel compounds described herein, such as of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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Paragraph 196-198
(2015/12/24)
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- Ligand-free Cu-catalyzed cyanation of aryl halides with K 4[Fe(Cn)6] in water
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A simple methodology for Cu-catalyzed cyanation of aryl halides with K 4[Fe(CN)6] was developed with water as the solvent in conjunction with ligand-free Cu(OAc)2·H2O as the catalyst. The suggested methodology i
- Ren, Yunlai,Zhao, Shuang,Tian, Xinzhe,Liu, Zhifei,Wang, Jianji,Yin, Weiping
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scheme or table
p. 564 - 567
(2010/04/23)
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- Microwave-enhanced and ligand-free copper-catalyzed cyanation of aryl halides with K4[Fe(CN)6] in water
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Copper-catalyzed cyanation of aryl halides was improved to be more economical and environmentally friendly by using water as the solvent and ligand-free Cu(OAc)2·H2O as the catalyst under microwave heating. The suggested methodology
- Ren, Yunlai,Wang, Wei,Zhao, Shuang,Tian, Xinzhe,Wang, Jianji,Yin, Weiping,Cheng, Lin
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supporting information; scheme or table
p. 4595 - 4597
(2009/10/18)
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- Tetrahydrobenzindole compounds
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A compound of formula (I) for use in the treatment or prevention of mental diseases A is N, CH, C having a double bond or CR5; each of B and Z is independently N, CH or CR1, with the proviso that A is N when B and/or Z is N; R1, R2, R3, R4and R5and n are as defined in the specification.
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Page column 24
(2010/02/05)
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- Sequential mono-N-arylation of piperazine nitrogens. Part 2: The role of hydrogen bonding
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A mechanistic study of the simple sequential N-arylation of piperazine suggests that in an electron-withdrawing group (EWG) containing N-arylated piperazines, hydrogen bonding of the secondary amine hydrogen is important for its non-metal catalyzed conversion to N,N'-diaryl piperazines. A combination of synthetic experiments, molecular modeling, and NMR studies were carried out to test this hypothesis.
- Eckert, Jeffrey,Chan, Tze-Ming,Osterman, Rebecca M.,Lambert, Joseph B.,Gala, Dinesh
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p. 5661 - 5665
(2007/10/03)
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