2371-26-8

Upstream product

• 105-39-5 chloroacetic acid ethyl ester 
• 95-64-7 4-amino-o-xylene 
• 105-36-2 ethyl bromoacetate 
• 924-44-7 glyoxylic acid ethyl ester 

Downstream Products

• 86323-99-1 [(3,4-Dimethyl-phenyl)-(3-mercapto-2-methyl-propionyl)-amino]-acetic acid 
• 669695-84-5 1-(3,4-dimethyl-phenyl)-imidazolidine-2,4-dione 

Relevant academic research and scientific papers

4-Pyridone-3-carboxylic acid as a benzoic acid bioisostere: Design, synthesis, and evaluation of EP300/CBP histone acetyltransferase inhibitors

Histone acetyltransferases (HATs) play a crucial role in post-translational modification. Among them, overexpression, mutation, or hyperfunction of EP300/CBP has been associated with various cancers. In this study, we identified the novel compound 2-chloro-5-[5-[(E)-[1-(3-chlorophenyl)-3-methyl-5-oxo-pyrazol-4-ylidene]methyl]-2-furyl]benzoic acid (1) as an EP300 HAT inhibitor via virtual screening. Further research has been focused on the design, synthesis, and in vitro biological evaluation of virtual hit derivatives. The studies revealed that 4-pyridone-3-carboxylic acid derivatives exhibited bioisosterism of benzoic acid. Replacement proved effective, providing compounds with similar EP300 HAT-inhibitory activity and improved cell growth-inhibitory activity compared to the benzoic acid analogs. Through these studies, we identified a potent and selective EP300/CBP HAT inhibitor.

N-substituted-3-[ 3-(substituted phenyl)-2-en-1-one]-4-hydroxy-pyrroline-2-ketone compound, preparation method and application

The invention discloses an N-substituent-3-[3-(substituted phenyl)-2-allyl-1- ketone]-4-hydroxypyrroline-2-ketone compound as well as a preparation method and application thereof, belonging to the technical field of organic synthesis and pesticides. The compound has a general structural formula (I). The N-substituent-3-[3-(substituent phenyl)-2-allyl-1- ketone]-4-hydroxypyrroline-2-ketone compound is synthesized from substituted phenylamine, ethyl chloroacetate, ethyl acetoacetate and substituted benzaldehyde. The compound has good tobacco mosaic virus resistant living body treatment activity and can be used for preparing plant virus resistant pesticides.

Enantioselective synthesis of arylglycine derivatives by direct C-H oxidative cross-coupling

A new method for the synthesis of chiral α-amino acid derivatives by enantioselective C-H arylation of N-aryl glycine esters with aryl boric acids in the presence of a chiral Pd(ii)-catalyst has been developed. This work successfully integrates the direct C-H oxidation with asymmetric arylation and exhibits excellent enantioselectivity. This journal is

Angiotensin converting enzyme inhibitors: N-substituted monocyclic and bicyclic amino acid derivatives

The synthesis of N-(3-mercaptopropionyl)-N-arylglycines (14a-x), -N-arylalanines (15a,b), -N-cycloalkylglycines (16a-k), and -1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids (17a-d), -1,2,3,4-tetrahydroquinoline-2-carboxylic acids (18a-f), and -indoline-2-carboxylic acids (19a-k) is described. In vitro inhibition of angiotensin converting enzyme (ACE) is reported for each compound, and the structure-activity relationship for each series is discussed. The in vivo inhibition of ACE and antihypertensive effects of representative compounds from each series are discussed. The most potent compound, 19d, had an in vitro ACE IC50 of 2.6 x 10-9 M and lowered blood pressure in spontaneous hypertensive rats 85 mm at a dose of 10 mg/kg po.