91131-23-6

Upstream product

• 89893-39-0 5-chloro-1-ethoxypent-1-yne 
• 1119-46-6 5-chloro-valeric acid 
• 62-53-3 aniline 
• 1575-61-7 5-Chlorovaleroyl chloride 

Downstream Products

• 142326-29-2 5-iodo-valeric acid anilide 
• 879216-05-4 5-azido-pentanoic acid phenylamide 
• 38560-30-4 1-(4-nitrophenyl)piperidine-2-one 
• 503615-03-0 3-(morpholin-4-yl)-1-(4-nitrophenyl)-5,6-dihydropyridin-2(1H)-one 
• 1267610-26-3 1-(4-aminophenyl)-3-(morpholin-4-yl)-5,6-dihydropyridin-2(1H)-one 
• 545445-44-1 5,6?dihydro?3?(4?morpholinyl)?1?[4?(2?oxo?1?piperidinyl)phenyl]?2(1H)?pyridone 
• 881386-01-2 3,3-dichloro-1-(4-nitrophenyl)piperidine-2-one 
• 503614-91-3 1-(4-methoxy-phenyl)-7-oxo-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid ethyl ester 
• 1643330-62-4 5-chloropentanoic acid [4-(5-morpholin-4-yl-6-oxo-3,6-dihydro-2H-pyridin-1-yl)phenyl]amide 
• 1432672-07-5 N-phenyl-5-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)pentanamide 
• 100134-63-2 5-cyano-N-phenylpentanamide 
• 100051-07-8 N-phenyl-pentamethylenediamine 
• 4789-09-7 1-phenylpiperidin-2-one 
• 159383-54-7 2-chloro-3-(3-chloro)propylquinoline 

Relevant academic research and scientific papers

Repurposing the 3-Isocyanobutanoic Acid Adenylation Enzyme SfaB for Versatile Amidation and Thioesterification

Genome mining of microbial natural products enables chemists not only to discover the bioactive molecules with novel skeletons, but also to identify the enzymes that catalyze diverse chemical reactions. Exploring the substrate promiscuity and catalytic mechanism of those biosynthetic enzymes facilitates the development of potential biocatalysts. SfaB is an acyl adenylate-forming enzyme that adenylates a unique building block, 3-isocyanobutanoic acid, in the biosynthetic pathway of the diisonitrile natural product SF2768 produced by Streptomyces thioluteus, and this AMP-ligase was demonstrated to accept a broad range of short-chain fatty acids (SCFAs). Herein, we repurpose SfaB to catalyze amidation or thioesterification between those SCFAs and various amine or thiol nucleophiles, thereby providing an alternative enzymatic approach to prepare the corresponding amides and thioesters in vitro.

PROCESS FOR THE PREPARATION OF APIXABAN AND INTERMEDIATES THEREOF

The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.

A method of preparing intermediates [...]

A disclosed preparation method for an apixaban intermediate comprises the following steps: step (1), performing an amidation reaction shown in the specification on a compound 3 and a compound M in an organic solvent under the effect of an organic alkali to obtain a reaction solution containing a compound 3'; and step (2), under the effect of an inorganic base, directly performing an nucleophilic substitution reaction shown in the specification on the reaction solution obtained in the step (1) to prepare a compound 4, and performing a nitration reaction on the compound 4 under the effect of concentrated sulfuric acid and concentrated nitric acid to prepare a compound 5. The preparation method provided by the invention is low in cost, simple in operation and suitable for industrialization.

COMPOUNDS AND METHODS

The present invention relates to compounds that inhibit histone deacetylase (HDAC) enzymes, the preparation of these compounds or salts of said compound, the use of these compounds in the treatment of neurodegenerative diseases or conditions ameliorated by inhibition of HDAC activity and pharmaceutical compositions that are comprised of these compounds.

New synthetic routes for N-substituted 1,n-diamines. II. Synthesis of selectively N-substituted tetra- and pentamethylenediamines from ω-alkanoic acid derivatives

A new approach for the synthesis of selectively N-substituted tetra- and pentamethylenediamines 1 (n = 4,5) is described. The method uses N-substituted ω-haloalkanamides 2 as precursors and involves the microwave-promoted conversion into ω-azidocarboxamides 3 and later the reduction of both azido and carboxamide groups with diborane.

Synthesis and electrochemical behavior of triazole-containing nicotinamide adenine dinucleotide analogs

The coupling of 2′,3′-di-O-acetyl nicotinamide mononucleotide with 3-butyn-1-ol in the presence of 2,4,6- triisopropylbenzenesulfonyl chloride quantitatively afforded a terminal alkyne-containing intermediate. Furthermore, copper(I)-mediated Huisgen [3 + 2] cycloaddition with a series of azido compounds in a two-phase solvent system gave eight triazole-containing nicotinamide adenine dinucleotide analogs with yields over 88%. The cyclic voltammetric behaviors of these novel analogs were investigated with a glassy carbon electrode, and structural features of these analogs on their electrochemical properties were briefly discussed.