- Fabrication of ω-Transaminase@Metal-Organic Framework Biocomposites for Efficiently Synthesizing Benzylamines and Pyridylmethylamines
-
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.
- Chen, Lina,Ding, Yingying,Jiao, Qingcai,Liu, Junzhong,Yu, Jinhai,Zhang, Hongjuan,Zong, Weilu
-
-
- N - methyl - 3 - ethyl - 4 - chlorine pyrazole derivative compounds
-
The invention discloses an N-methyl-3-ethyl-4-hlorine pyrrole derivative compound with insecticidal/acaricidal activities and an isomer thereof shown in formula (I) and formula (II) and a preparation method thereof. The N-methyl-3-ethyl-4-hlorine pyrrole derivative compound has the insecticidal/acaricidal activities and is used for controlling armyworms, aphids and mites on crops, and the formulations of the N-methyl-3-ethyl-4-hlorine pyrrole derivative compound comprise a concentrated emulsion, missible oil, a suspending agent and wettable powder.
- -
-
Paragraph 0057; 0058; 0060
(2017/07/19)
-
- Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors
-
Cancer metabolism and epigenetics are among the most intensely pursued research areas in anticancer drug discovery. Here we report the first small molecules that simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and histone deacetylase (HDAC), two important targets of cancer metabolism and epigenetics, respectively. Through iterative structure-based drug design, chemical synthesis, and biological assays, a highly potent dual NAMPT and HDAC inhibitor was successfully identified. Compound 35 possessed excellent and balanced activities against both NAMPT (IC50 = 31 nM) and HDAC1 (IC50 = 55 nM). It could effectively induce cell apoptosis and autophagy and ultimately led to cell death. Importantly, compound 35 showed excellent in vivo antitumor efficacy in the HCT116 xenograft model. This proof-of-concept study demonstrates the feasibility of discovering an inhibitor targeting cancer metabolism and epigenetics and provides an efficient strategy for multitarget antitumor drug discovery.
- Dong, Guoqiang,Chen, Wei,Wang, Xia,Yang, Xinglin,Xu, Tianying,Wang, Pei,Zhang, Wannian,Rao, Yu,Miao, Chaoyu,Sheng, Chunquan
-
p. 7965 - 7983
(2017/10/18)
-
- Pyridine methylamino pyridine compound and method for preparing the same
-
The invention discloses a picolinate amino pyridine compound which is shown in the formula (I) and has sterilizing, insect/mite killing and weeding bioactivity as well as a preparation method thereof, a sterilizing, insect/mite killing and weeding herbicide composition containing the compound, and an application and method for controlling fungi, insects/mites and weeds by using the compound.
- -
-
-
- A N-(2 - (3 - (trifluoromethyl) phenoxy) - 4-pyridyl) a method for the synthesis of imines (by machine translation)
-
This invention involves a kind of N-(2 the [...] (3 the [...] (trifluoromethyl) phenoxy) - 4 the [...] pyridyl) methylimine synthesis method, which belongs to the field of chemical synthesis. Traditional production N-(2 the [...] (3 the [...] (trifluoromethyl) phenoxy) - 4 the [...] pyridyl) methylimine process backwardness, long flow path, the yield is low, a large amount of the three wastes, it is difficult to control. The present invention provides a mild reaction conditions, the high yield of N-(2 the [...] (3 the [...] (trifluoromethyl) phenoxy) - 4 the [...] pyridyl) methylimine synthetic method. (by machine translation)
- -
-
Paragraph 0004; 0007
(2016/11/02)
-
- 5-LIPOXYGENASE INHIBITORS
-
The present invention relates to pyrazole derivatives of formula 1 and to process as for their synthesis as 5-lipoxygenase (5-LO) inhibitors. The present invention also relates to pharmacological compositions containing these pyrazole derivatives, as well as, methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, Type I diabetes, psoriasis, allograft rejection, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis, allergic rhinitis and other inflammatory and/or autoimmune disorders.
- -
-
Page/Page column 58
(2012/01/13)
-
- PROCESS FOR PRODUCING SUBSTITUTED METHYLAMINE COMPOUND AND TRIAZINE DERIVATIVE
-
The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid. (wherein A represents an organic group that is either a hydrocarbon group or a heterocyclic group, or said organic group that has a substituent, R represents a hydrogen atom, an organic group that is either a hydrocarbon group or a heterocyclic group, or said organic group that has a substituent, L represents a halogen atom and the like, and n represents an integer of 2 to 20)
- -
-
Page/Page column 17
(2010/01/29)
-
- PROCESS FOR PRODUCING SUBSTITUTED METHYLAMINE COMPOUND AND TRIAZINE DERIVATIVE
-
The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid. (wherein A represents an organic group that is either a hydrocarbon group or a heterocyclic group, or said organic group that has a substituent, R represents a hydrogen atom, an organic group that is either a hydrocarbon group or a heterocyclic group, or said organic group that has a substituent, L represents a halogen atom and the like, and n represents an integer of 2 to 20)
- -
-
Page/Page column 9
(2010/06/11)
-
- Synthesis, herbicidal activities, and 3D-QSAR of 2-cyanoacrylates containing aromatic methylamine moieties
-
A series of novel 2-cyanoacrylates containing different aromatic rings were synthesized, and their structures were characterized by 1H NMR, elemental analysis, and single-crystal X-ray diffraction analysis. Their herbicidal activities against four weeds and inhibition of photosynthetic electron transport against isolated chloroplasts (the Hill reaction) were evaluated. Both in vivo and in vitro data showed that the compounds containing benzene, pyridine, and thiazole moieties gave higher activities than those containing pyrimidine, pyridazine, furan, and tetrahedronfuran moieties. To further explore the comprehensive structure-activity relationship on the basis of in vitro data, comparative molecular field analysis (CoMFA) was performed, and the results showed that a bulky and electronegative group around the para-position of the aromatic rings would have the potential for higher activity, which offered important structural insights into designing highly active compounds prior to the next synthesis.
- Liu, Yu-Xiu,Wei, Deng-Guo,Zhu, Ye-Rong,Liu, Shao-Hua,Zhang, Yong-Lin,Zhao, Qi-Qi,Cai, Bao-Li,Li, Yong-Hong,Song, Hai-Bin,Liu, Ying,Wang, Yong,Huang, Run-Qiu,Wang, Qing-Min
-
experimental part
p. 204 - 212
(2009/04/11)
-
- Practical synthesis of (6-chloro-3-pyridyl)methylamine by highly selective hydrogenation of 6-chloro-3-pyridinecarbonitrile with improved Raney nickel catalyst
-
A practical synthesis of (6-chloro-3-pyridyl)methylamine (1), one of the key intermediates of neo-nicotinoid insecticides, by a highly selective hydrogenation of 6-chloro-3-pyridinecarbonitrile (4) is described. The use of an improved Raney nickel catalyst, prepared from an alloy of low nickel content (Ni 38%, A1 62%) and subjected to heat treatment in water (98 °C, 2 h) after leaching of aluminum, was highly effective for the selective hydrogenation of 4. The hydrogenation of 4 using this catalyst was carried out in EtOH-H2O [6:1 (v/v)] and NH3 at 50 °C and 1.2-1.4 kg cm-2 hydrogen pressure to give 1 in 86% yield and 3-pyridylmethylamine, a dechlorinated by-product, in 2% yield.
- Tanaka, Ken,Nagasawa, Minoru,Sakamura, Hideki
-
p. 1227 - 1231
(2007/10/03)
-
- Highly selective hydrogenation of 2-chloro-5-cyanopyridine with an improved sponge nickel catalyst
-
A practical synthesis of (6-chloropyridin-3-yl)methylamine (1), a key intermediate of neo-nicotinoide insecticides 2, was achieved by highly selective hydrogenation of 2-chloro-5-cyanopyridine (3). The hydrogenation of 3 with an improved Sponge nickel catalyst, prepared from an alloy of low nickel content (Ni 38%, Al 62%) and subjected to heat treatment in water, was carried out at 50°C and 1.2-1.4 kg/cm2 hydrogen pressure to give 1 in 86% yield and (pyridin-3-yl)methylamine (4), a dechlorinated by-product, in only 2% yield.
- Tanaka, Ken,Nagasawa, Minoru,Kasuga, Yuzo,Sakamura, Hideki,Takuma, Yuki,Iwatani, Katsuyoshi
-
p. 5885 - 5888
(2007/10/03)
-
- Method for manufacturing 3-(aminomethyl)-6-chloropyridines
-
The present invention is directed to methods for manufacturing 3-(aminomethyl)-6-chloropyridines represented by a general formula ?II!; STR1 wherein R2 represents hydrogen or a lower alkyl and R3 represents hydrogen, a lower alkyl or an halogen atom, characterized in that the compound represented by the general formula ?II! is manufactured by allowing 3-(substituted-aminomethyl)pyridine 1-oxide represented by a general formula ?I!; STR2 wherein R1 represents alkyl, aryl, aralkyl or alkoxy, R2 and R3 are as described above, to react with a base represented by a general formula ?a!; wherein R', R" and R'" may be the same or different one another and represent each independently a lower alkyl or an aromatic group, or R', R" , R'" and N may form together an optionally-substituted pyridine ring, in the presence of an electrophilic reagent having at least one chlorine atom, and subsequently treating the reaction product with hydrogen chloride and water. The compounds manufactured according to the present invention are useful as the raw materials used for the manufacturing of agricultural chemicals and pharmaceuticals, and particularly useful for the raw materials for manufacturing insecticides.
- -
-
-
- Butenone compounds, their preparation and their use as pesticides
-
A butenone compound having the general formula I: STR1 wherein R1 represents a pyridyl or thiazolyl group bearing one or more substituents independantly selected from halogen atoms, alkyl, alkoxy, alkylthio, haloalkyl, cyano, alkoxycarbonyl, alkylamino and dialkylamino; R2 represents a hydrogen atom, an alkyl group or an alkylcarbonyl group; R3 represents an alkyl group; R4 represents a haloalkyl group; X represents a sulphur atom or a group of formula N--R5, wherein R5 represents a hydrogen atom, an alkyl group or an alkylcarbonyl group; and n is 0 or 1, methods for their preparation and their use in combating pests.
- -
-
-
- Tetrahydropyrimidines, their production and use
-
There is provided a pest control composition containing a compound represented by the formula, STR1 wherein R1, R2, R3 and R4 are the same or different and independently mean a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted and X means an electron attracting group or a salt thereof. The compounds are of minimal toxicity to man, domestic animals and fish and selectively display remarkable control effect on pests.
- -
-
-
- Guanidine derivatives, their production and insecticides
-
An insecticidal composition containing a guanidine derivative of the formula: STR1 wherein R1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R2 is a hydrogen atom or an optionally substituted hydrocarbon group, R3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R1 is an optionally substituted heterocyclic group or a salt thereof.
- -
-
-