63609-01-8Relevant academic research and scientific papers
Metal- and additive-free cascade trifluoroethylation/cyclization of organic isoselenocyanates by phenyl(2,2,2-trifluoroethyl)iodonium triflate
Zhao, Cheng-Long,Shi, Jin,Lu, Xiuqiang,Wu, Xun,Zhang, Cheng-Pan
supporting information, (2019/09/03)
A novel and convenient cascade trifluoroethylation/cyclization of organic isoselenocyanates by phenyl(2,2,2-trifluoroethyl)iodonium triflate is reported. A series of 2-isoselenocyanobiaryls and aryl alkyl isoselenocyanates reacted with phenyl(2,2,2-trifluoroethyl)iodonium triflate in CH2Cl2 at 40 °C under metal- and additive-free conditions for 3 h to provide the corresponding trifluoroethylselenolated phenanthridines and 3,4-dihydroisoquinoline derivatives in good to excellent yields. The reaction represents the first general approach to access trifluoroethylselenolated phenanthridines and 3,4-dihydroisoquinolines from organic isoselenocyanates.
One-Step Transformation of Trichloroacetamide into Isonitrile
Adachi, Masaatsu,Miyasaka, Tadachika,Hashimoto, Honoka,Nishikawa, Toshio
supporting information, p. 380 - 383 (2017/04/24)
A one-step transformation of trichloroacetamide, a protective group for the amine function, into isonitrile was successfully developed. The substrate scope and functional group tolerance of this procedure are also described.
Iodide-Catalyzed Synthesis of Secondary Thiocarbamates from Isocyanides and Thiosulfonates
Mampuys, Pieter,Zhu, Yanping,Sergeyev, Sergey,Ruijter, Eelco,Orru, Romano V. A.,Van Doorslaer, Sabine,Maes, Bert U. W.
supporting information, p. 2808 - 2811 (2016/07/06)
A new method for the synthesis of secondary thiocarbamates from readily available isocyanides and thiosulfonates with broad functional group tolerance is reported. The reaction proceeds under mild reaction conditions in isopropanol and is catalyzed by inexpensive sodium iodide.
TREATMENT AND DIAGNOSIS OF CANCER AND PRECANCEROUS CONDITIONS USING PDE10A INHIBITORS AND METHODS TO MEASURE PDE10A EXPRESSION
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Paragraph 0137, (2015/02/02)
Disclosed are methods for treating cancer and precancerous conditions with PDE10A specific inhibitors and diagnosis of neoplastic diseases based on elevated levels of PDE10A.
Novel ultrasound-promoted parallel synthesis of trifluoroatrolactamide library via a one-pot passerini/hydrolysis reaction sequence and their fungicidal activities
Yu, Shu-Jing,Zhu, Cong,Bian, Qiang,Cui, Can,Du, Xiu-Jiang,Li, Zheng-Ming,Zhao, Wei-Guang
supporting information, p. 17 - 23 (2014/02/14)
An ultrasound-promoted one-pot Passerini/hydrolysis reaction sequence has been developed for the synthesis of trifluoroatrolactamide derivatives using a diverse range of trifluoroacetophenones and isonitriles in acetic acid. Parallel synthesis in a centrifuge tube using a noncontact ultrasonic cell crusher was used in this study as an efficient method for the rapid generation of combinatorial trifluoroatrolactamide libraries, and subsequent biochemical evaluation of the resulting compounds indicated that they possessed excellent broad-spectrum fungicidal activities. N-(4-chlorophenyl)-2-(4-ethylphenyl)-3,3, 3-trifluoro-2-hydroxypropanamide and N-(4-chlorophenyl)-3,3,3-trifluoro-2- hydroxy-2-(4-methoxyphenyl)propanamide, in particular, showed significant fungicidal activities against all of the fungal species tested in the current study.
A general simple methodology for synthesis of isonitriles using benzene-1,3-disulfonyl dichloride
Ghorbani-Vaghei, Ramin,Amiri, Mostafa,Veisi, Hojat
, p. 37 - 41 (2013/07/26)
Isonitrile derivatives have been synthesized in good to high yields by dehydration of aliphatic and aromatic formamides in the presence of benzene-1,3-disulfonyl dichloride as easy and efficient reagent.
A synthesis of dihydroimidazo[5,1-a]isoquinolines using a sequential Ugi-Bischler-Napieralski reaction sequence
Seganish, W. Michael,Bercovici, Ana,Ho, Ginny D.,Loozen, Hubert J.J.,Timmers, Cornelis M.,Tulshian, Deen
scheme or table, p. 903 - 905 (2012/03/10)
A flexible route to analogues of dihydroimidazo[5,1-a]isoquinolines is described. The synthesis hinges on a sequential Ugi coupling, followed by a Bischler-Napieralski reaction to form the imidazole isoquinoline core. This route facilitates the introduction of a range of substitutions throughout the carbon framework.
The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia
Ho, Ginny D.,Michael Seganish,Bercovici, Ana,Tulshian, Deen,Greenlee, William J.,Van Rijn, Rachel,Hruza, Alan,Xiao, Li,Rindgen, Diane,Mullins, Deborra,Guzzi, Mario,Zhang, Xiaoping,Bleickardt, Carina,Hodgson, Robert
scheme or table, p. 2585 - 2589 (2012/05/05)
The identification of potent and orally active dihydroimidazoisoquinolines as PDE 10A inhibitors is reported. The SAR development led to the discovery of compound 35 as a potent, selective, and orally active PDE10A inhibitor. Compound 35 inhibited MK-801-induced hyperactivity at 3 mg/kg and displayed a 10-fold separation between the minimal effective doses for inhibition of MK-801-induced hyperactivity and hypolocomotion in rats.
DIHYDROIMIDAZOISOQUINOLINE DERIVATIVES USEFUL AS PDE10 INHIBITORS
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Page/Page column 17, (2011/02/24)
The present invention relates to dihydroimidazoisoquinolines and derivatives thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.
Microwave-assisted synthesis of isonitriles: A general simple methodology
Porcheddu, Andrea,Giacomelli, Giampaolo,Salaris, Margherita
, p. 2361 - 2363 (2007/10/03)
(Chemical Equation Presented) A facile conversion of formamides to isonitriles under very mild conditions and microwave irradiation is described. This simple and efficient method has been applied for the synthesis of both aliphatic and aromatic isonitriles in high yields.
