30923-65-0

Upstream product

• 765-43-5 Cyclopropyl methyl ketone 
• 93-89-0 benzoic acid ethyl ester 
• 98-88-4 benzoyl chloride 
• 2868-37-3 methyl cyclopropylcarboxylate 
• 98-86-2 acetophenone 
• 1083010-55-2 3-cyclopropyl-1-phenylprop-2-yn-1-one 
• 354996-72-8 (1H-benzo[d][1,2,3]triazol-1-yl)(cyclopropyl)methanone 

Downstream Products

• 1208127-10-9 5-cyclopropyl-3-phenyl-1H-pyrazole 
• 34650-69-6 1-cyclopropyl-2-phenylethane-1,2-dione 

Relevant academic research and scientific papers

PIKFYVE KINASE INHIBITORS

The present invention relates to compounds useful as inhibitors of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) as well as their use for treating diseases and disorders associated with PIKfyve.

Non-metal catalytic method for preparing 1,3-diketone compounds based on acetyenic ketone

The invention discloses a non-metal catalytic method for preparing 1,3-diketone compounds based on acetyenic ketone. The preparation method is a stepwise method or a one-pot method. The stepwise method comprises the following steps: mixing an acetyenic ketone compound I, a nitrogen-containing aromatic compound II and a No.1 base for a reaction, performing separation and purification to obtain an intermediate product, mixing the intermediate product and a No.2 base for a reaction, and performing separation and purification to obtain the product; and the one-pot method comprises the following steps: firstly mixing an acetyenic ketone compound I and a nitrogen-containing aromatic compound II, adding a No.1 base, performing a reaction for a period of time, adding a No.2 base, continuing a reaction for a period of time, and finally performing separation and purification to obtain the product. The method provided by the invention has mild reaction conditions, simple operation and a higher yield, wherein the yield is generally 80% or more, and the method has greater practical application value in drug synthesis.

Method for synthesizing 1, 3-dicarbonyl compound based on terminal alkyne and acyl halide by one-pot process

The invention belongs to the technical field of catalytic synthesis, and discloses a method for synthesizing a 1, 3-dicarbonyl compound by a one-pot process, and the method comprises the following steps: by using simple palladium and copper salts as catalysts, reacting terminal alkyne with acyl halide at 0-80 DEG C for 0.5-12 hours under the action of trifluoromethanesulfonic acid to obtain the 1,3-dicarbonyl compound, wherein the molar ratio of the terminal alkyne to the acyl halide to the palladium salt to the copper salt to the trifluoromethanesulfonic acid is 1 to (1 to 2) to (0.00001 to0.10) to (0.00001 to 0.10) to (0.00004 to 0.40); the catalysts used in the method are common the commercialized palladium salt and copper salt, reagents used in the reaction are commercialized reagents, in addition, the raw materials are cheap and easy to obtain, functional group tolerance is good, reaction conditions are mild, operation is easy and convenient, and atom economy is high.

Method of preparing 1,3-diketone compound by acetyenic ketone

The invention relates to a preparation method of preparing a 1,3-diketone compound by acetyenic ketone. The preparation method comprises the following steps: S1, putting alpha-alkynyl ketone compound,water, gold salt and silver salt in a reaction solvent to obtain a precursor mixture, wherein the molar ratio of the alpha-alkynyl ketone compound, water, gold salt and silver salt is 1: (1-50): (0.001-0.10): (0.002-0.15); and S2, putting the precursor mixture obtained in the S1 to react at a reaction temperature of 0-50 DEG C to obtain the 1,3-diketone compound, wherein the reaction time is 5 min to 48 h. The method is simple in reaction condition, free of acid or alkaline additives and high in yield, and can be applied to modern production on a large scale.

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)

We report the discovery and medicinal chemistry optimization of a novel series of pyrazole-based inhibitors of human lactate dehydrogenase (LDH). Utilization of a quantitative high-throughput screening paradigm facilitated hit identification, while structure-based design and multiparameter optimization enabled the development of compounds with potent enzymatic and cell-based inhibition of LDH enzymatic activity. Lead compounds such as 63 exhibit low nM inhibition of both LDHA and LDHB, submicromolar inhibition of lactate production, and inhibition of glycolysis in MiaPaCa2 pancreatic cancer and A673 sarcoma cells. Moreover, robust target engagement of LDHA by lead compounds was demonstrated using the cellular thermal shift assay (CETSA), and drug-target residence time was determined via SPR. Analysis of these data suggests that drug-target residence time (off-rate) may be an important attribute to consider for obtaining potent cell-based inhibition of this cancer metabolism target.

PROCESS FOR THE PREPARATION OF 1,3-DICARBONYL COMPOUNDS

The condensation reaction of a ketone with either an ester or a carbonate to form, respectively, a 1,3-diketone or a beta -ketoester often affords poor results under the standard condensation reaction conditions. High yields and high purities of the desired product can be obtained by performing the reaction using an alkoxide base in DMSO as the sole solvent.

Process for the preparation of 1,3-dicarbonyl compounds

The condensation reaction of a ketone with either an ester or a carbonate to form, respectively, a 1,3-diketone or a beta -ketoester often affords poor results under the standard condensation reaction conditions. High yields and high purities of the desir

3,5-Cycloalkyl pyrazolium salts as fungicides

There is provided a method for the control of plant pathogenic fungi with certain 3(5) or 3,5-cycloalkyl pyrazolium salts and to a method of protecting plants from fungal attack by applying to the foliage of said plants said pyrazolium salt in fungicidall