104774-81-4

Upstream product

• 16714-23-1 2-azido-benzoic acid methyl ester 
• 89431-22-1 ethyl prop-2-ynyl methylphosphonate 
• 134-20-3 2-carbomethoxyaniline 
• 814-68-6 acryloyl chloride 

Downstream Products

• 1146206-16-7 C₂₃H₂₀N₂O₄ 
• 1229020-95-4 C₃₀H₄₇N₃O₄ 

Relevant academic research and scientific papers

Concurrent pathway and unexpected products in the CuAAC reaction of ethyl prop-2-ynyl methylphosphonate with aromatic azides

[Figure not available: see fulltext.] The CuI-mediated click reaction of aromatic azides, containing the carboxyl moiety in the ortho position to the azido group, with ethyl prop-2-ynyl methylphosphonate proceeded via a concurrent pathway whereby the form

Synthesis of 4-Trifluoromethylated 1,3-Butadienes via Palladium Catalyzed Heck Reaction

1,3-Butadiene plays a key role in modern synthetic chemistry and biochemistry because it is a key intermediate in the synthesis of many drugs. A new and effective method for the synthesis of 4-trifluoromethylated 1,3-butadiene through the fluorinated Heck reaction catalyzed by Pd(0) is described. Without additives, 1-chloro-3,3,3-trifluoropropene (an inexpensive CF3 structural unit that is harmless to ozone) reacts with enamide to synthesize 4-trifluoromethylated 1,3-butadienes with good yield, high regioselectivity and chemical selectivity, and strong tolerance of substrate functional groups such as alkynes, aldehyde, and ester groups.

Pyrazole derivative for FGFR inhibitor and preparation method of pyrazole derivative

The invention provides a pyrazole derivative for an FGFR inhibitor and a preparation method of the pyrazole derivative. The invention specifically relates to an amide pyrazole compound serving as an FGFR irreversible inhibitor, and a preparation method and application thereof. The present invention provides a compound as shown in Formula I, or a pharmaceutically acceptable salt, or solvate, isotope substitute, prodrug, or metabolite thereof. The compound as shown in general formula I have FGFR inhibitory activity, and is capable of preventing or treating disorders associated with FGFR activityor expression, preferably such as cancer.

O-amino aromatic amide derivative as well as preparation method and application thereof

The invention discloses an o-amino aromatic amide derivative as well as a preparation method and application thereof. The o-amino aromatic amide derivative is a compound with a structural general formula I, II and III or a pharmaceutically acceptable salt

Systematic study of the glutathione (GSH) reactivity of N-arylacrylamides: 1. Effects of aryl substitution

Success in the design of targeted covalent inhibitors depends in part on a knowledge of the factors influencing electrophile reactivity. In an effort to further develop an understanding of structure-reactivity relationships among N-arylacrylamides, we determined glutathione (GSH) reaction rates for a family of N-arylacrylamides independently substituted at ortho-, meta-, and para-positions with 11 different groups common to inhibitor design. We find that substituent effects on reaction rates show a linear Hammett correlation for ortho-, meta-, and para-substitution. In addition, we note a correlation between 1H and 13C NMR chemical shifts of the acrylamide with GSH reaction rates, suggesting that NMR chemical shifts may be a convenient surrogate measure of relative acrylamide reactivity. Density functional theory calculations reveal a correlation between computed activation parameters and experimentally determined reaction rates, validating the use of such methodology for the screening of synthetic candidates in a prospective fashion.

Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B

Structural optimization and preliminary structure-activity relationship studies of a series of N-substituted maleimide fused-pyrazole analogues with Cdc25B inhibitory activity, starting from a high-throughput screening hit, are illustrated. A simplified 3,5-diacyl pyrazole analogue was obtained as the most potent compound (118, IC50 = 0.12 μM) with a 270-fold increase in potency.

N-PHENYLAMIDE DERIVATIVE, PROCESS FOR THE PREPARATION THEREOF, AND COMPOSITION FOR PREVENTING OR TREATING ISCHEMIC DISEASES COMPRISING SAME

The present invention relates to a compound of Formula I, a process for the preparation thereof, and a composition for preventing or treating an ischemic disease comprising a compound of Formula I' as an effective ingredient. Since the N-phenylamide derivatives of the present invention can significantly reduce ischemic cell death, they can be effectively used for preventing or treating ischemic diseases mediated by ischemic cell death, or for protecting organs.