23612-57-9

Usage

Uses

Used in Pharmaceutical Industry:
(2-Aminopyridin-3-yl)methanol is used as an intermediate in the synthesis of mirtazapine, an antidepressant medication. Its role in the production of mirtazapine is crucial, as it serves as a building block for the final drug molecule, helping to alleviate symptoms of depression and improve the quality of life for patients suffering from this condition.
Chemical Properties:
(2-Aminopyridin-3-yl)methanol exhibits a light yellow crystalline appearance, which is indicative of its solid state at room temperature. The presence of the amino group and the hydroxyl group in its molecular structure endows it with specific reactivity and solubility properties, making it a valuable compound for further chemical modifications and applications in the pharmaceutical sector.

InChI:InChI=1/C6H8N2O/c7-6-5(4-9)2-1-3-8-6/h1-3,9H,4H2,(H2,7,8)

Upstream product

• 504-29-0 2-aminopyridine 
• 86847-64-5 N-(3-formyl-2-pyridinyl)-2,2-dimethylpropanamide 
• 5345-47-1 2-aminopyridin-3-carboxylic acid 
• 13362-26-0 2-aminopyridine-3-carboxylic acid ethyl ester 

Downstream Products

• 858431-27-3 3-(chloromethyl)pyridin-2-amine, hydrochloride salt 
• 861046-07-3 2-methyl-1,2,3,4-tetrahydro-1,8-naphthyridine 
• 274676-47-0 7-methyl-1,2,3,4-tetrahydro-[1,8]naphthyridine 
• 15936-02-4 2-phenyl-1,8-naphthyridine 
• 65182-54-9 2-(4'-methoxyphenyl)-1,8-naphthyridine 
• 65182-60-7 2-(4-chlorophenyl)-1,8-naphthyridine 
• 58309-20-9 3-methyl-2-phenyl-1,8-naphthyridine 
• 1309205-48-8 6-[(1E)-3-oxo-3-(3-phenoxypyrrolidin-1-yl)prop-1-en-1-yl]-3,4-dihydro-1,8-naphthyridin-2(1H)-one 
• 1309205-47-7 6-[(1E)-3-{[3-(4-fluorophenoxy)methyl]piperidin-1-yl}-3-oxoprop-1-en-1-yl]-3,4-dihydro-1,8-naphthyridin-2(1H)-one 
• 1309205-45-5 6-[(1E)-3-oxo-3-(2-phenylpyrrolidin-1-yl)prop-1-en-1-yl]-3,4-dihydro-1,8-naphthyridin-2(1H)-one 
• 1309205-42-2 (E)-6-(3-oxo-3-(3-phenoxyazetidin-1-yl)prop-1-en-1-yl)-3,4-dihydro-1,8-naphthyridin-2(1H)-one 
• 1309205-40-0 6-[(1E)-3-{[4-(4-fluorophenoxy)methyl]piperidin-1-yl}-3-oxoprop-1-en-1-yl]-3,4-dihydro-1,8-naphthyridin-2(1H)-one 
• 1309206-51-6 1'-methyl-6-((E)-3-oxo-3-(3-((E)-1-(benzyloxyimino)ethyl)azetidin-1-yl)prop-1-enyl)-1H-spiro[[1,8]naphthyridine-3,4'-piperidin]-2(4H)-one 
• 1309208-28-3 (E)-4-(4-methoxybenzyl)-7-(3-oxo-3-(3-(thiophen-2-ylmethoxy)azetidin-1-yl)prop-1-enyl)-4,5-dihydro-1H-pyrido[2,3-e][1,4]diazepin-2(3H)-one 

Relevant academic research and scientific papers

6H-THIENO[2,3-E][1,2,4]TRIAZOLO[3,4-C][1,2,4]TRIAZEPINE DERIVATIVE

The 6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,2,4]triazepine derivatives or salts thereof of the present invention have BRD4 inhibitory activity, and thus, they are useful as medicaments, in particular, as prophylaxis and/or therapeutic agents for diseases associated with BRD4.

Alkenyl compound and its method and use thereof

The invention provides a new substituted alkenyl compound, pharmaceutically acceptable salts of the new substituted alkenyl compound, a medicinal preparation of the new substituted alkenyl compound, and application of the new substituted alkenyl compound, the pharmaceutically acceptable salts and the medicinal preparation of the new substituted alkenyl compound in aspects of regulating the activity of protein kinase and regulating the intercellular or intracellular signal response. The invention also relates to a medicament composition containing the compound at the same time, and relates to a method for treating high-proliferative diseases of mammals especially the human by using the medicament composition.

MACROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS

Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

Method for preparing 2-amino-3-hydroxymethylpyridine

The invention discloses a method for preparing 2-amino-3-hydroxymethylpyridine, and belongs to the field of chemical synthesis. 2-aminopyridine and pivaloyl chloride are used as initial reactants to form intermediate product 2-pivalamidopyridine under the action of triethylamine, after hydrogen extraction by use of n-butyllithium, dimethylformamide is added for hydroformylation, and target product2-amino-3-hydroxymethylpyridine can be obtained by reduction with sodium borohydride. Raw materials used in the method are low in cost, and the method is simple in operation, short in synthesis process, mild in reaction conditions, high in yield, and suitable for large-scale industrial production.

A rice the nitrogen is mellow synthetic method

The invention discloses a 1-(3-hydroxymethylpyridine-2-yl)-4-methyl-2-phenylpiperazine synthesis method. The method includes: dissolving N-(2-chloroethyl)-N-methyl-alpha-chlorine-beta phenethylamine in mixed solution of water and a nonpolar solvent to obtain solution A, and dissolving 2-amino-3-hydroxymethylpyridine into a nonpolar solvent containing a small quantity of low carbon alcohols to obtain solution B; dripping the solution B into the solution A to obtain an intermediate by reaction, dissolving the intermediate into an anhydrous high-boiling-point polar solvent, and dripping into an anhydrous high-boiling-point polar solvent of inorganic iodides under inert gas shielding to realize reaction for obtaining 1-(3-hydroxymethylpyridine-2-yl)-4-methyl-2-phenylpiperazine. By two steps for synthesis of 1-(3-hydroxymethylpyridine-2-yl)-4-methyl-2-phenylpiperazine, oxidization of the intermediate due to direct high-temperature reaction can be avoided by specific solvent systems, and reaction stability and yield are improved.

ALKENYL COMPOUNDS AND METHODS OF USE

The present invention provides novel substituted alkenyl compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS

The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors. Formula(I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

NOVEL HETEROCYCLIC ACRYLAMIDES AND THEIR USE AS PHARMACEUTICALS

The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.

Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors

Tumor cells extensively utilize the pentose phosphate pathway for the synthesis of ribose. Transketolase is a key enzyme in this pathway and has been suggested as a target for inhibition in the treatment of cancer. In a pharmacodynamic study, nude mice with xenografted HCT-116 tumors were dosed with 1 ('N3′-pyridyl thiamine'; 3-(6-methyl-2-amino-pyridin-3-ylmethyl)-5-(2-hydroxy-ethyl)-4-methyl-thiazol-3-ium chloride hydrochloride), an analog of thiamine, the co-factor of transketolase. Transketolase activity was almost completely suppressed in blood, spleen, and tumor cells, but there was little effect on the activity of the other thiamine-utilizing enzymes α-ketoglutarate dehydrogenase or glucose-6-phosphate dehydrogenase. Synthesis and SAR of transketolase inhibitors is described.

NOVEL SUBSTITUTED IMIDAZOLE DERIVATIVES

The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1', R2, R2', R3, R3', R4, and R4', which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8', which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.