50264-88-5Relevant academic research and scientific papers
Late-stage Pd-catalyzed Cyanations of Aryl/Heteroaryl Halides in Aqueous Micellar Media
Thakore, Ruchita R.,Takale, Balaram S.,Singhania, Vani,Gallou, Fabrice,Lipshutz, Bruce H.
, p. 212 - 216 (2020/12/01)
New technology is described that enables late stage ppm Pd-catalyzed cyanations of highly complex molecules, as well as a wide variety of aryl and heteroaryl halides possessing sensitive functional groups. These reactions are efficient in water containing nanomicelles, formed from a commercially available and inexpensive surfactant. The implications for advancing drug synthesis and discovery are apparent.
A convenient reagent for the conversion of aldoximes into nitriles and isonitriles
Zhang, Wei,Lin, Jin-Hong,Zhang, Pengfei,Xiao, Ji-Chang
supporting information, p. 6221 - 6224 (2020/06/29)
For the dehydroxylation of aldoximes with 4-nitro-1-((trifluoromethyl)sulfonyl)-imidazole (NTSI), slight modifications of reaction conditions resulted in significantly different reaction paths to provide either nitriles or isonitriles. The challenging conversion of aldoximes into isonitriles was achieved under mild conditions.
Thiocyanate radical mediated dehydration of aldoximes with visible light and air
Ban, Yong-Liang,Dai, Jian-Ling,Jin, Xiao-Ling,Zhang, Qing-Bao,Liu, Qiang
supporting information, p. 9701 - 9704 (2019/08/15)
We developed a new means of activating aldoximes by an in situ generated thiocyanate radical from ammonium thiocyanate and molecular oxygen at room temperature. With a catalytic amount of organic dye aizenuranine as the photocatalyst, the dehydration of aldoximes proceeds smoothly under visible light irradiation, providing a simple to handle, excellent functional group tolerance, and metal-free protocol for a wide range of nitriles.
Access to 1: H -indazoles, 1 H -benzoindazoles and 1 H -azaindazoles from (het)aryl azides: A one-pot Staudinger-aza-Wittig reaction leading to N-N bond formation?
Alaime,Daniel,Hiebel,Pasquinet,Suzenet,Guillaumet
supporting information, p. 8411 - 8414 (2018/08/06)
The synthesis of various substituted 1H-indazoles is reported through N-N bond formation from an iminophosphorane derivative. Supported by control experiments, an original Staudinger-aza-Wittig tandem mechanism is proposed for this transformation.
A general, practical palladium-catalyzed cyanation of (hetero)aryl chlorides and bromides
Senecal, Todd D.,Shu, Wei,Buchwald, Stephen L.
supporting information, p. 10035 - 10039 (2013/10/01)
Playing it safe: The nontoxic cyanide source K4[Fe(CN) 6]×3 H2O can be used for the cyanation of (hetero)aryl halides. The application of palladacycle catalysts prevents poisoning during catalyst formation, thereby allowing for low catalyst loadings, fast reaction times, and wide heterocyclic substrate scope.
NITROGENATED HETEROCYCLIC COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 18; 23, (2008/12/06)
The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I): wherein Y1 represents N or C(R4) ; Y2 represents N or C(R5) ; R4 and R5 independently represent an alkyl group, a hydrogen atom etc. ; one of R1 and R2 represents an optionally substituted aryl group, an alkoxygroup or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyanogroup, ahalogenatometc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.
NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
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Page/Page column 64, (2008/12/05)
Compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein X, R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
