40134-18-7Relevant academic research and scientific papers
Preparation method of 2-chloro-N, N-dimethyl nicotinamide
-
Paragraph 0010; 0025-0026; 0028-0029; 0031-0032, (2021/03/13)
The invention belongs to the technical field of pesticides, and particularly relates to a preparation method of 2-chloro-N, N-dimethyl nicotinamide. The preparation method of the 2-chloro-N, N-dimethyl nicotinamide comprises the following steps of taking 2-chloronicotinic acid as a raw material, and carrying out esterification reaction with methanol to obtain 2-chloronicotinic acid methyl ester, and carrying out aminolysis reaction with dimethylamine in the presence of a catalyst N, N-dimethyl nicotinamide to obtain the 2-chloro-N, N-dimethyl nicotinamide. The preparation method disclosed by the invention is mild and controllable in reaction, simple in process equipment, low in dimethylamine consumption, low in production cost and good in product quality, and the amount of wastewater is greatly reduced and is easy to treat.
LIBRARIES OF PYRIDINE-CONTAINING MACROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING THE SAME
-
Paragraph 00221, (2019/01/11)
The present disclosure relates to novel pyridine-containing macrocyclic compounds and libraries thereof that are useful as research tools for drug discovery efforts. This disclosure also relates to methods of preparing these compounds and libraries and methods of using these libraries, such as in high throughput screening. In particular, these libraries are useful for evaluation of bioactivity at existing and newly identified pharmacologically relevant targets, including G protein-coupled receptors, nuclear receptors, enzymes, ion channels, transporters, transcription factors, protein-protein interactions and nucleic acid-protein interactions. As such, these libraries can be applied to the search for new pharmaceutical agents for the treatment and prevention of a range of medical conditions.
Towards new sila- Or germa-derivatives of motesanib
Boddaert, Thomas,Querolle, Olivier,Meerpoel, Lieven,Angibaud, Patrick,Maddaluno, Jacques,Durandetti, Muriel
, p. 1210 - 1218 (2019/07/31)
– Developing new access to original silylated heterocycles is an emerging challenge in medicinal chemistry. In this paper, we describe a synthesis of silylated and germylated Motesanib analogues relying on a peptide coupling between a nicotinic acid derivative and silylated or germylated heterocycles, prepared according to our previous reports.
A ultrasonic process for synthesizing 2 - halogenated nicotinate and intermediates thereof
-
Paragraph 0057; 0058; 0061, (2018/04/21)
The invention discloses a method for synthesizing 2-halogenated ester nicotinate and a 2-halogenated ester nicotinate intermediate according to an ultrasonic method. The method comprises the following steps: adding substituent amino acrolein, a catalyst and cyanacetic ester into a reactor for a reaction under ultrasonic radiation; tracing the reaction till substituent amino acrolein is disappeared, thereby obtaining a reaction solution I containing the 2-halogenated ester nicotinate intermediate; then, adding halogen hydride into the reaction solution I for another reaction to obtain a reaction solution II; tracing and monitoring the reaction till completion; adding a lye into the reaction solution II to adjust the pH value of the reaction solution II to be 5-6; carrying out standing stratification to obtain a water layer and an organic layer; conducting extraction on the water layer by utilizing an organic solvent, and then combining the extraction solution with the organic layer; carrying out refining to obtain 2-halogenated ester nicotinate. Through the adoption of the method, an organic synthesis reaction can be effectively facilitated, the reaction speed and yield can be improved, and the environmental protection can be promoted; the reaction time is short and the operation is simple, that is, the organic synthesis reaction can be finished within 2 hours in general; the product yield and quality are high; specifically, the product yield can reach 90% or higher, and exceed that achieved according to the conventional solvent heating reflux method.
A microwave synthesis 2 - halogenated nicotinate and intermediates thereof
-
Paragraph 0034; 0035, (2018/05/16)
The invention discloses a method for synthesizing 2-halogenated nicotinic acid ester and intermediates thereof through microwave method. The method comprises the following steps: adding substitute amino acrolein, a catalyst and cyan-acetic ester into a reactor, carrying out reaction under microwave radiation, and tracking the reaction till substitute amino acrolein disappears to prepare and obtain reaction liquid of the intermediates of 2-halogenated nicotinic acid ester; adding hydrogen halide into the reaction liquid, continuously carrying out reaction, and tracking and monitoring the reaction till the reaction is complete; adding alkali liquor into the reaction liquid to adjust the pH value to 5-6; carrying out standing delamination to obtain an aqueous layer and an organic layer; extracting the aqueous layer with an organic solvent, combining the extracted aqueous layer with the organic layer, and carrying out refinement to prepare and obtain 2-halogenated nicotinic acid ester. The synthesis method of 2-halogenated nicotinic acid ester related to the invention has the advantages of beingenvironment-friendly, short in reaction time, simple to operate, high in product yield and good in quality.
A fluorine-containing tetrazine pyridine compound and its use
-
Paragraph 0010; 0029; 0030, (2017/08/25)
The invention provides fluorine-containing tetrazine pyridine compounds disclosed as Formula I. The compounds have ultrahigh inhibiting and killing actions on harmful acarids and acarid ova, and can be used as an acaricide for controlling acarid harm in agriculture and forestry.
An ionic liquid method of synthesizing 2 - halogenated nicotinate and intermediates thereof
-
Paragraph 0060; 0061; 0062, (2017/10/13)
The invention discloses a method for synthesizing 2-halogenated nicotinate and an intermediate thereof through an ionic liquid method. The method comprises the steps that cyan-acetic ester, ionic liquid and substituted amino acrolein are evenly mixed and heated to a preset temperature for conducting a reaction, the reaction is tracked till the substituted amino acrolein disappears, reaction liquid is cooled to the room temperature and extracted for multiple times through organic solvents, the residual phase of the ionic liquid is reused after being washed and dried, and the intermediate of the 2-halogenated nicotinate is obtained by evaporating the organic solvents from the organic phase; when the 2-halogenated nicotinate is synthesized, the organic solvents do not need to be separated from the intermediate of the 2-halogenated nicotinate, the reaction is continuously conducted by adding hydrogen halide into the organic phase, and the tracking monitoring is conducted till the reaction is completed; the 2-halogenated nicotinate product is prepared after separation. The synthesizing method of the 2-halogenated nicotinate has the advantages of being green and environmentally friendly, easy to operate, high in product yield and good in quality of the synthesized product.
Method using hydrothermal method to synthesize 2-halogeneated nicotinate and 2-halogeneated nicotinic acid
-
Paragraph 0031; 0032, (2017/11/01)
The invention discloses a method using a hydrothermal method to synthesize 2-halogeneated nicotinate and 2-halogeneated nicotinic acid and relates to the field of chemical synthesizing. The method uses substituted amino acrolein, catalyst, catalyst assistant, water and cyanoacetate as raw materials to synthesize the 2-halogeneated nicotinate and the 2-halogeneated nicotinic acid through the hydrothermal method. Compared with the prior art, the method is environmentally friendly, easy in separation, high in product yield, good in product quality, capable of achieving large-scale industrial production favorably, and the like.
RING-FUSED 2-PYRIDONE DERIVATIVES AND HERBICIDES
-
Page/Page column 72-73, (2011/12/12)
Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C═O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.
Claisen condensation of N-methylpyrrolidinone and α-chloronicotinic esters
Kaminski, Thomas,Kirsch, Gilbert
, p. 229 - 234 (2008/09/19)
Reaction between α-halo-nicotinic esters and a nucleophilic source such as the N-methylpyrrolidin-2-one (NMP) gave unexpected results. The presence of the halide on the pyridine gave a very interesting migration reaction. Extension to 6-methylnicotinic ester derivatives lead to an unexpected carbanion condensation.
