23459-35-0Relevant articles and documents
Alkyl Radical Addition to Aliphatic and Aromatic N-Acylhydrazones Using an Organic Photoredox Catalyst
Cullen, Stephen T. J.,Friestad, Gregory K.
, p. 8290 - 8294 (2019)
Increased versatility of intermolecular radical addition to imino acceptors via photoredox catalysis is reported. Primary and secondary radicals, generated via visible-light photocatalysis from alkyl biscatecholatosilicates with organocatalyst 4CzIPN, add
Catalytic asymmetric oxidative carbonylation-induced kinetic resolution of sterically hindered benzylamines to chiral isoindolinones
Mu, Qiu-Qi,Nie, Yi-Xue,Li, Hang,Bai, Xing-Feng,Liu, Xue-Wei,Xu, Zheng,Xu, Li-Wen
supporting information, p. 1778 - 1781 (2021/02/27)
A highly enantioselective kinetic resolution of sterically hindered benzylamines has been achieved for the first time through transition-metal-catalyzed oxidative carbonylation, in which the new KR strategy offered a new approach to afford chiral isoindolinones (er up to 97?:?3) and the origin of chemoselectivity and stereoselectivity was confirmed by density functional theory (DFT) calculations.
Method for synthesizing chiral amine compound
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Paragraph 0064; 0071-0073; 0129-0131, (2019/10/01)
The present invention provides a method for synthesizing a chiral amine compound. The method comprises the following steps: (1) reacting a compound of formula I with t-butylsulfonamide in the presenceof a catalyst to obtain a compound having a structure represented by formula II; 2) reacting the compound of the formula II in a hydrogen atmosphere in the presence of an iridium catalyst and a ligand to obtain a compound of formula III; and (3) carrying out a t-butylsulfonyl group removal reaction on the compound of the formula III to obtain the chiral amine compound. The method constructs the structure of sulfonamide by a keto carbonylgroup, and synthesizes the chiral amine compound with the aralkylamine structure by an asymmetric catalytic hydrogenation reaction of the sulfonamide structure, the ee value is generally 80% or above, the highest ee value is 99% or above, the yield of each step reaction can reach 90% or above, and the total yield is high.
Method for synthesizing dextral alpha-cyclohexylbenzylamine
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Paragraph 0006; 0009, (2017/07/01)
The invention discloses a method for synthesizing dextral alpha-cyclohexylbenzylamine. The method comprises synthesizing racemic alpha-cyclohexylbenzylamine through catalytic reduction of cyclohexyl phenyl ketone in the presence of a reduction catalyst, and carrying out dynamic kinetic resolution on alpha-cyclohexylbenzylamine under combined action of lipase and a racemization catalyst to obtain alpha-cyclohexylbenzylamine. The method has the characteristics of simple operation, wide raw material source, good product yield and high optical purity of the resolution product.
PROCESS FOR THE PREPARATION OF CHIRAL AMINES FROM PROCHIRAL KETONES
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Page/Page column 5; 6, (2015/12/11)
There is provided a method for the preparation of an enantiomerically enriched amine from a prochiral ketone.
APPLICATIONS OF N6-SUBSTITUTED ADENOSINE DERIVATIVE AND N6-SUBSTITUTED ADENINE DERIVATIVE TO CALMING, HYPNOSES, CONVULSION RESISTANCE, EPILEPTIC RESISTANCE, PARKINSON DISEASE RESISTANCE, AND DEMENTIA PREVENTION AND TREATMENT
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, (2018/10/27)
PROBLEM TO BE SOLVED: To prepare analgesics, hypnotic agents, anticonvulsant agents, antiepileptics, antiparkinson drugs, dementia prophylactics, and health care food. SOLUTION: The present invention relates to an N6-substituted adenosine derivative and an N6-substituted adenine derivative selected from the group consisting of specific compounds. The present invention also relates to a pharmaceutical composition at least comprising a therapeutically effective amount of the compounds and a pharmaceutically acceptable carrier. The invention further relates to the compounds used in preparation of analgesics, hypnotic agents, anticonvulsant agents, antiepileptics, antiparkinson drugs, dementia prophylactics, and health care food. COPYRIGHT: (C)2016,JPO&INPIT
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides
Laufer, Radoslaw,Ng, Grace,Liu, Yong,Patel, Narendra Kumar B.,Edwards, Louise G.,Lang, Yunhui,Li, Sze-Wan,Feher, Miklos,Awrey, Don E.,Leung, Genie,Beletskaya, Irina,Plotnikova, Olga,Mason, Jacqueline M.,Hodgson, Richard,Wei, Xin,Mao, Guodong,Luo, Xunyi,Huang, Ping,Green, Erin,Kiarash, Reza,Lin, Dan Chi-Chia,Harris-Brandts, Marees,Ban, Fuqiang,Nadeem, Vincent,Mak, Tak W.,Pan, Guohua J.,Qiu, Wei,Chirgadze, Nickolay Y.,Pauls, Henry W.
, p. 4968 - 4997 (2014/10/16)
TTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and acetamido moieties at positions 3 and 5, respectively, establishing a novel chemical class culminating in identification of 72 (CFI-400936). This potent inhibitor of TTK (IC50 = 3.6 nM) demonstrated good activity in cell based assay and selectivity against a panel of human kinases. A co-complex TTK X-ray crystal structure and results of a xenograft study with TTK inhibitors from this class are described.
INDAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 69; 75; 123, (2013/04/25)
The present teaching provide indazole compounds represented by Structural Formulae (I) or (I') or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as T
A versatile Ru catalyst for the asymmetric transfer hydrogenation of both aromatic and aliphatic sulfinylimines
Pablo, Oscar,Guijarro, David,Kovacs, Gabor,Lledos, Agusti,Ujaque, Gregori,Yus, Miguel
, p. 1969 - 1983 (2012/03/26)
A highly efficient Ru catalyst based on an achiral, very simple, and inexpensive amino alcohol ligand (2-amino-2-methylpropan-1-ol) has been developed for the asymmetric transfer hydrogenation (ATH) of chiral N-(tert-butylsulfinyl)imines. This complex is able to catalyze the ATH of both aromatic and the most challenging aliphatic sulfinylimines by using isopropyl alcohol as the hydrogen source. The diastereoselective reduction of aromatic, heteroaromatic, and aliphatic sulfinylketimines, including sterically congested cases, over short reaction times (1-4 h), followed by desulfinylation of the nitrogen atom, affords the corresponding highly enantiomerically enriched (ee up to >99%) α-branched primary amines in excellent yields. The same ligand was equally effective for the synthesis of both (R)- and (S)-amines by using the appropriate absolute configuration in the iminic substrate. DFT mechanistic studies show that the hydrogen-transfer process is stepwise. Moreover, the origin of the diastereoselectivity has been rationalized.
KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 100, (2011/10/31)
The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are a pharmaceutical composition and method of use thereof.