6967-51-7Relevant academic research and scientific papers
Fabrication of ω-Transaminase@Metal-Organic Framework Biocomposites for Efficiently Synthesizing Benzylamines and Pyridylmethylamines
Yu, Jinhai,Zong, Weilu,Ding, Yingying,Liu, Junzhong,Chen, Lina,Zhang, Hongjuan,Jiao, Qingcai
, p. 380 - 390 (2021/11/05)
In this study, ten ω-transaminases (ω-TAs) have been investigated to efficiently catalyze the synthesis of twenty-four functionalized benzylamines and pyridylmethylamines. We optimized the reactions, screened suitable amino donors and compared ω-transaminases activities for all aromatic aldehyde substrates. Under the optimized conditions, eighteen aromatic amines have been obtained with 60.4%–96.6% conversions and isolated only via simple extraction and recrystallization with 18.5%–81% yields on a preparative scale. Furthermore, we first immobilized the Bm-STA onto the MOFs via the physical adsorption to overcome the limitation of free enzyme and improve their industrial applications. The obtained Bm-STA/UiO-66-NH2 composites exhibited not only high enzymes loading (80.4 mg g?1) and enzyme activity recovery (95.8%), but also the better reusability, storage stability, pH stability and the tolerance to acetone and DMF.
In silico design and synthesis of N-arylalkanyl 2-naphthamides as a new class of non-purine xanthine oxidase inhibitors
Ho, Sheau Ling,Lin, Ching-Ting,Lee, Shoei-Sheng
, p. 789 - 801 (2021/01/12)
A series of N-arylalkanyl 2-naphthamides (Xa~e), which were predicted from virtual molecular docking on a built xanthine oxidase template as potential inhibitors, were synthesized. Their inhibitory activity against xanthine oxidase was assayed. Among these prepared, compounds Xb (IC50 13.6?μM), Xc (IC50 13.1?μM), and Xd (IC50 12.5?μM) showed comparable inhibitory activity to allopurinol (IC50 22.1?μM). The in vitro assay result correlated well with molecular docking scores, ΔG?=??16.99, ?17.66, and ?17.13 Kcal/mol, respectively. On the potassium oxonate-induced hyperuricemic mice model, oral administration of Xc-Ac (40 mg/ Kg), the per-O-acetylated Xc, could reduce the blood uric acid level by 60% in comparison to the normal control group and is statistically significant (p .01) while compared with the hyperuricemic mice group.
Hydrogenation of Aliphatic and Aromatic Nitriles Using a Defined Ruthenium PNP Pincer Catalyst
Neumann, Jacob,Bornschein, Christoph,Jiao, Haijun,Junge, Kathrin,Beller, Matthias
supporting information, p. 5944 - 5948 (2015/09/22)
Selective catalytic reductions of nitriles are presented using the commercially available Ru-Macho-BH complex. A variety of aliphatic, aromatic and (hetero)cyclic nitriles including industrially important adipodinitrile are hydrogenated to the corresponding primary amines. Modelling suggests the reaction follows an outer sphere hydrogenation mechanism. An efficient and selective catalytic reduction of nitriles is presented using the commercially available Ru-Macho-BH complex. A variety of aliphatic, aromatic and (hetero)cyclic nitriles including the industrially important adipodinitrile are hydrogenated to the corresponding primary amines. The reaction follows an outer-sphere mechanism.
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
-
Paragraph 0122, (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
Sodium nitrite-catalyzed aerobic oxidative Csp2-Csp3 coupling: Direct construction of the 4-aryldihydroisoquinolinone moiety
Su, Bo,Deng, Meng,Wang, Qingmin
, p. 977 - 981 (2014/04/03)
A bioinspired approach for the construction of the 4- aryldihydroisoquinolinone moiety via direct oxidative Csp2-Csp 3 coupling has been developed, which uses inexpensive sodium nitrite as catalyst and environmentally benign oxygen in the air as terminal oxidant.
TBAF-catalyzed hydrosilylation for the reduction of aromatic nitriles
Bornschein, Christoph,Werkmeister, Svenja,Junge, Kathrin,Beller, Matthias
supporting information, p. 2061 - 2065 (2013/10/08)
The selective catalytic hydrosilylation of functional groups is becoming an interesting tool for organic synthesis. In the present study, fluoride-catalyzed hydrosilylations of aromatic nitriles have been examined in detail. Using catalytic amounts of inexpensive tetra-n-butylammonium fluoride (TBAF) various aromatic nitriles are reduced in good yields under mild conditions.
N6-SUBSTITUTED ADENOSINE DERIVATIVES AND N6-SUBSTITUTED ADENINE DERIVATIVES AND USES THEREOF
-
Paragraph 0185, (2013/03/26)
The present invention provides N6-substituted adenosine derivatives and N6-substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.
N6-SUBSTITUTED ADENOSINE DERIVATIVES, N6-SUBSTITUTED ADENINE DERIVATIVES AND USES THEREOF
-
, (2012/11/06)
The present invention provides N6-substituted adenosine derivatives and N6-substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.
3(2H)pyridazinone, process for its preparation and anti-allergic agent containing it
-
, (2008/06/13)
A 3(2H)pyridazinone of the formula: STR1 wherein R1 is C2 -C5 alkyl; R2 is hydrogen, C1 -C3 alkyl, chlorine or bromine; R3 is hydrogen or C1 -C4 alkyl; and each of Y1, Y2 and Y3 which may be the same or different, is hydrogen, C1 -C8 alkyl, C2 -C8 alkenyl, halogen, --(CH2)l A [wherein A is substituted amino of the formula --N(R4) (R5) (wherein each of R4 and R5 which may be the same or different, is C1 -C4 alkyl, or R4 and R5 together form C4 -C6 alkylene), morpholino, 4-R6 -piperazin-1-yl (wherein R6 is C1 -C3 alkyl) or --OR7 (wherein R7 is hydrogen or C1 -C3 alkyl), and l is an integer of 0 to 3], --OR8 [wherein R8 is hydrogen, C1 -C8 alkyl, C3 -C5 alkenyl, benzyl or --(CH2)q --R9 [wherein R9 is CO2 R3 (wherein R3 is as defined above), --CONHR3 (wherein R3 is as defined above) or --CH2 OR7 (wherein R7 is as defined above), and q is an integer of 1 to 5]], --CO2 R3 (wherein R3 is as defined above), --CON(R10) (R11) [wherein each of R10 and R11 which may be the same or different, is hydrogen, C1 -C4 alkyl or C3 -C5 alkenyl, or R10 and R11 together form C4 -C6 alkylene, --(CH2)2 O(CH2)2 -- or --(CH2)2 N(R6)(CH2)2 -- (wherein R6 is as defined above)], --CONH(CH2)m A (wherein A is as defined above, and m is an integer of 2 to 4), --CH=CHCOR12 (wherein R12 is hydroxy, C1 -C4 alkoxy or --N(R13) (CH2)n CO2 R3 (wherein R13 is hydrogen, C1 -C6 alkyl or cycloalkyl, R3 is as defined above, and n is an integer of 1 to 4)), --SR14 (wherein R14 is C1 -C4 alkyl), --CN or STR2 wherein R3 is as defined above), or two of Y1, Y2 and Y3 together form STR3 (wherein p is an integer of 1 or 2), and a pharmaceutically acceptable salt thereof.
3(2H)Pyridazinone, process for its preparation and anti-allergic agent containing it
-
, (2008/06/13)
A 3(2H)pyridazinone of the formula: STR1 wherein R1 is hydrogen, methyl, C3 -C6 alkenyl, C5 or C6 cycloalkyl, benzyl, phenyl, --(CH2)m CO2 R3 (wherein R3 is hydrogen or C1 -C5 alkyl, and m is an integer of from 1 to 4), --(CH2)n A (wherein A is --OH or --N(R4)2 wherein R4 is C1 -C3 alkyl, and n is an integer of from 2 to 6) or --CH2 CF3 ; R2 is chlorine or bromine; each of Y1 and Y2 which may be the same or different, is hydrogen, C1 -C5 alkyl, C2 -C8 alkenyl, halogen, --OR5 (wherein R5 is hydrogen, C1 -C8 alkyl or STR2 wherein q is an integer of from 1 to 4), --CO2 R6 (wherein R6 is hydrogen or C1 -C5 alkyl), --N(R7)2 (wherein R7 is C1 -C4 alkyl) or --SR8 (wherein R8 is C1 -C4 alkyl); and Y3 is C1 -C5 alkyl, C2 -C8 alkenyl, halogen, --OR5 (wherein R5 is as defined above), --CO2 R6 (wherein R6 is as defined above), --N(R7)2 (wherein R7 is as defined above) or --SR8 (wherein R8 is as defined above), or a pharmaceutically acceptable salt thereof.
