4664-00-0Relevant articles and documents
Method for preparing 6,7-dihydro-5H-pyrrolo-pyridine hydrochloride
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Paragraph 0020-0022, (2017/10/31)
The invention discloses a preparation method for preparing 6,7-dihydro-5H-pyrrolo-pyridine hydrochloride. The method is characterized in that a target product 6,7-dihydro-5H-pyrrolo-pyridine hydrochloride is obtained through lactamization, reduction and salifying by taking furo[3,4-b]pyridine-5,7-dione as an original raw material. The compound is an important medical intermediate.
Method for preparing 6-(1-phenyl-ethyl)-pyrrolo[3,4-b]pyridine-5,7-dione
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Paragraph 0016, (2017/05/26)
The invention more specifically relates to a method for preparing 6-(1-phenyl-ethyl)-pyrrolo[3,4-b]pyridine-5,7-dione. The preparation method comprises the following steps: 5H-pyrrolo[3,4-b]pyridine-5,7(6H)-dione is generated from 2,3-dipicolinic acid and urea, ethylbenzene and hydrogen halide are reacted in order to generate (1-haloethyl)benzene, (1-haloethyl)benzene and 2,3-dipicolinic acid are generated into a crude product, and finally a target compound is obtained by chiral separation. The method is advantageous in that the synthesis technology has the advantages of mild reaction condition, short reaction time, high yield without generation of harmful refuses, simple post-treatment, recycling of 1,2-dichloroethane solvent which is separated from the reaction process, and easy industrialization.
(S, S) - 2,8-diazabicyclo [4.3.0] nonane preparation method
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Paragraph 0077; 0078, (2017/02/09)
The invention relates to a novel preparation method of (S,S)-2,8-diazabicyclo[4.3.0]. The method comprises the steps that: 2,3-pyridine dicarboxylic acid derivative and amide are subjected to condensation, such that 2,3-pyridine dicarboximide is formed; 2,3-pyridine dicarboximide is subjected to protection and hydrogenation reduction, such that 8-substituted-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane is produced; the product is reduced in a borohydride reduction system, such that 8-substituted-2,8-diazabicyclo[4.3.0]nonane is obtained; the product is subjected to optical-active organic acid resolution, such that 8-site protection group is removed, and the final product is obtained. Or, 2,3-pyridine dicarboximide is directly subjected to hydrogenation reduction, such that 7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane is produced; the product is directly reduced in a borohydride reduction system, such that 2,8-diazabicyclo[4.3.0]nonane is produced; the 2,8-diazabicyclo[4.3.0]nonane is subjected to optical-active organic acid resolution, such that the final product is directly obtained. The method provided by the invention is advantaged in simple reaction route. The raw materials are cheap and easy to obtain. The reaction conditions are mild and easy to control. The method is suitable for industrialized productions.
New artificial fluoro-cofactor of hydride transfer with novel fluorescence assay for redox biocatalysis
Zhang, Lei,Yuan, Jun,Xu, Yufang,Zhang, Y.-H. Percival,Qian, Xuhong
supporting information, p. 6471 - 6474 (2016/06/06)
A new artificial fluoro-cofactor was developed for the replacement of natural cofactors NAD(P), exhibiting a high hydride transfer ability. More importantly, we established a new and fast screening method for the evaluation of the properties of artificial cofactors based on the fluorescence assay and visible color change.
Synthetic method of 6-(1-phenyl-ethyl)-pyrrolo[3,4-b]pyridyl-5,7-dione
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Paragraph 0013; 0014; 0015, (2017/07/21)
The invention particularly relates to a synthetic method of 6-(1-phenyl-ethyl)-pyrrolo[3,4-b]pyridyl-5,7-dione. The synthetic method is characterized in that 2,3-pyridinedicarboxylic acid and urea are subjected to melt reaction to produce amide, then amide reacts with methylbenzylamine to produce a crude product 6-(1-phenyl-ethyl)-pyrrolo[3,4-b]pyridyl-5,7-dione which is subjected to chiral resolution to obtain the target product 6-(1-phenyl-ethyl)-pyrrolo[3,4-b]pyridyl-5,7-dione. The synthetic method has the advantages that the reaction steps are simple and short, the reaction is quick, no by-product is produced, environmental pollution is reduced, the reaction yield is high, the separation efficiency of a chiral chromatographic column is relatively high, and the product purity is improved.
Pyridine salt / 1,4-dihydropyridine derivative and preparation method thereof
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Paragraph 0149; 0150; 0151, (2016/10/09)
The present invention discloses a pyridine salt / 1,4-dihydropyridine derivative (NAD / NADH analog) with novel structure. The NAD / NADH analog can substitute natural NAD / NADH to be applied to a biochemical system for redox reactions, and can also be used as an electron carrier for the energy transfer of an enzymatic fuel cell. Further, the NAD / NADH analogs provided by the invention are easy to prepare, isolate and purify, and have a high yield.
Zinc-catalyzed selective reduction of cyclic imides with hydrosilanes: Synthesis of ω-hydroxylactams
Ding, Guangni,Lu, Bin,Li, Yuyuan,Wan, Jun,Zhang, Zhaoguo,Xie, Xiaomin
supporting information, p. 1013 - 1021 (2015/03/30)
Cyclic imides were selectively reduced to the corresponding ω-hydroxylactams in high yields with (EtO)3SiH (triethoxysilane) or PMHS (polymethylhydrosiloxane) under catalysis of zinc diacetate dehydrate [Zn(OAc)2 2H2O] (10%) and tetramethylethylenediamine (TMEDA) (10%). This catalytic protocol showed good functional group tolerance as well as excellent regioselectivity for unsymmetrical imides bearing coordinating groups adjacent to the carbonyl.
Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2
Galli, Ubaldina,Mesenzani, Ornella,Coppo, Camilla,Sorba, Giovanni,Canonico, Pier Luigi,Tron, Gian Cesare,Genazzani, Armando A.
, p. 58 - 66,9 (2020/07/31)
As part of an effort to identify novel selective modulators of sirtuins, we synthesized and tested several isosteres and constrained analogues of nicotinamide. Biological data suggest that compound 2 is selective for Sirt3 over Sirt1 and Sirt2.
New efficient access to fused (Het)Aryltetrahydroindolizinones via N-acyl iminium intermediates
Chiurato, Matteo,Boulahjar, Rajaa,Routier, Sylvain,Troin, Yves,Guillaumet, Gérald
scheme or table, p. 4647 - 4653 (2010/07/05)
In this paper, we described the preparation of fused (Het)Aryltetrahydroindolizinones via N-acyl iminium intermediates. Two different routes were also explored to achieve the synthesis. The first one consists in the intramolecular reaction of β-hydroxylactams whereas the second route one is an intermolecular condensation between a 2-formylester or a β-alkoxylactone and an appropriate primary amine. We also developed two heterocyclic strategies to obtain the adequate unavailable starting materials in pyridine, pyrazine, quinoline, and quinaxoline series and then perform all inter or intramolecular reactions. Scope and limitations are given.
Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors
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Page/Page column 60, (2010/02/10)
Certain aza- and polyaza-naphthalenyl ketones including certain quinolinyl and naphthyridinyl ketones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment or the delay in the onset of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
