1452-15-9Relevant 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 (2021)
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.
CHIRAL INDOLE COMPOUNDS AND THEIR USE
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Paragraph 0062; 00248; 00249, (2020/10/28)
The present disclosure relates to indole compounds of Structural Formula 2 and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer. Formula (II)
Corresponding amine nitrile and method of manufacturing thereof
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Paragraph 0150; 0151; 0152; 0162, (2018/05/07)
The invention relates to a manufacturing method of nitrile. Compared with the prior art, the manufacturing method has the characteristics of significantly reduced using amount of an ammonia source, low environmental pressure, low energy consumption, low production cost, high purity and yield of a nitrile product and the like, and nitrile with a more complex structure can be obtained. The invention also relates to a method for manufacturing corresponding amine from nitrile.
NOVEL TETRAHYDROPYRIDOPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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Page/Page column 42; 43, (2018/05/24)
The present invention provides novel compounds having the general formula: wherein R1, R2 and R3 are as described herein, compositions including the compounds and methods of using the compounds.
Mild palladium-catalyzed cyanation of (hetero)aryl halides and triflates in aqueous media
Cohen, Daniel T.,Buchwald, Stephen L.
supporting information, p. 202 - 205 (2015/01/30)
A mild, efficient, and low-temperature palladium-catalyzed cyanation of (hetero)aryl halides and triflates is reported. Previous palladium-catalyzed cyanations of (hetero)aryl halides have required higher temperatures to achieve good catalytic activity. This current reaction allows the cyanation of a general scope of (hetero)aryl halides and triflates at 2-5 mol % catalyst loadings with temperatures ranging from rt to 40 °C. This mild method was applied to the synthesis of lersivirine, a reverse transcriptase inhibitor.
Virtually instantaneous, room-temperature [11C]-cyanation using biaryl phosphine Pd(0) complexes
Lee, Hong Geun,Milner, Phillip J.,Placzek, Michael S.,Buchwald, Stephen L.,Hooker, Jacob M.
supporting information, p. 648 - 651 (2015/01/30)
A new radiosynthetic protocol for the preparation of [11C]aryl nitriles has been developed. This process is based on the direct reaction of in situ prepared L·Pd(Ar)X complexes (L = biaryl phosphine) with [11C]HCN. The strategy is operationally simple, exhibits a remarkably wide substrate scope with short reaction times, and demonstrates superior reactivity compared to previously reported systems. With this procedure, a variety of [11C]nitrile-containing pharmaceuticals were prepared with high radiochemical efficiency.
Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors
Chen, Fei,Chai, Hui,Su, Ming-Bo,Zhang, Yang-Ming,Li, Jia,Xie, Xin,Nan, Fa-Jun
supporting information, p. 628 - 633 (2014/07/07)
Inspired by the thiazole-thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clinical symptoms of EAE mice.
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.
Propylphosphonic anhydride (T3P): A remarkably efficient reagent for the one-pot transformation of aromatic, heteroaromatic, and aliphatic aldehydes to nitriles
Augustine, John Kallikat,Atta, Rajendra Nath,Ramappa, Balakrishna Kolathur,Boodappa, Chandrakantha
experimental part, p. 3378 - 3382 (2010/03/03)
Propylphosphonic anhydride has been demonstrated to be an efficient reagent for the transformation of aromatic, heteroaromatic, and aliphatic aldehydes to respective nitriles in excellent yields. This procedure offers simple and one-pot access to nitriles and highlights the synthetic utility of T3P as a versatile reagent in organic chemistry. Georg Thieme Verlag Stuttgart - New York.
N-PHENYLAMIDINES AS 5-HT2A RECEPTOR ANTAGONISTS
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Page/Page column 7; 8, (2008/06/13)
Compounds of formula (I), are 5-HT2A receptor antagonists, and hence find use in treatment of a variety of adverse conditions of the 10 central nervous system.
