74530-59-9

Upstream product

• 136637-38-2 5-(2-methoxyacetyl)-2,2-dimethyl-1,3-dioxane-4,6-dione 
• 75-65-0 tert-butyl alcohol 
• 31059-08-2 1-(1H-imidazol-1-yl)-2-methoxyethanone 
• 104197-11-7 magnesium salt of tert-butyl hydrogen malonate 
• 540-88-5 acetic acid tert-butyl ester 
• 6290-49-9 methyl methoxyacetate 

Downstream Products

• 158120-50-4 1-(4-chloro-phenyl)-5-methoxymethyl-1H-pyrazole-4-carboxylic acid 
• 1616278-56-8 tert-butyl (5-(5-(2,4-difluorobenzyl)-1,3,4-thiadiazol-2-yl)-2-(ethylcarbamoyl)-3-methoxy-4-oxopyridin-1(4H)-yl)(methyl)carbamate 
• 1616278-55-7 C₂₇H₃₀F₂N₄O₄S 
• 1616278-54-6 C₂₇H₃₀F₂N₄O₄S 
• 1616278-44-4 C₂₅H₂₅F₂N₅O₄S 
• 1616278-43-3 C₂₅H₂₃F₂N₅O₅S 
• 1616278-42-2 C₂₆H₂₅F₂N₅O₅S 
• 1616278-41-1 C₂₅H₂₃F₂N₅O₅S 
• 1616278-40-0 C₂₂H₂₃F₂N₅O₅S 
• 1616278-39-7 C₂₂H₂₂F₂N₄O₆S 
• 1616278-38-6 C₂₄H₂₆F₂N₄O₆S 
• 1616277-96-3 ethyl 5-(5-(2,4-difluorobenzyl)-1,3,4-thiadiazol-2-yl)-3-methoxy-4-oxo-4H-pyran-2-carboxylate 
• 1369958-89-3 ((R)-7-(3,4-dichlorophenyl)-5-(methoxymethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone 

Relevant academic research and scientific papers

Synthesis method of 4-methoxy-3-tert-butyl oxobutyrate

The invention provides a synthesis method of 4-methoxy-3-tert-butyl -oxobutyrate, and the method comprises the following steps: S1, reacting methoxyacetic acid with CDI at 0-20 DEG C under the protection of nitrogen to generate acylimidazole; S2, dissolving mono-tert-butyl malonate in a solvent, dropwise adding an isopropyl Grignard agent under an ice bath condition, and reacting at -10 to 25 DEGC to generate mono-tert-butyl malonate magnesium salt; and S3, dropwise adding the solution obtained after the reaction in the S2 into the solution obtained after the reaction in the S1, and after dropwise adding is completed, carrying out a reaction for 15-18 hours at the temperature of 20-35 DEG C to generate the 4-methoxy-3-tert-butyl oxobutyrate. In conclusion, the methoxyacetic acid and the mono-tert-butyl malonate are adopted as raw materials and are easy to obtain and cheap, flammable and explosive reagents are not used in the whole synthesis process, the reaction condition temperatureis mild, aftertreatment is little, the yield is high, and in conclusion, the synthesis method is low in cost, high in efficiency, mild in reaction condition and suitable for large-scale industrial production.

SPIROCYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS

The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R11 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

SPIROCYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS

Disclosed are Spirocyclic Heterocycle Compounds of Formula (I) and pharmaceutically acceptable salts thereof, where A, B, X, Y, R1, R2 and R11 are as defined herein. Composition comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject are also disclosed.

4-PYRIDINONETRIAZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS

The present invention relates to 4-Pyridinonetriazine Derivatives of Formula (I); and pharmaceutically acceptable salts thereof, wherein A, X, Y, R1, R2, R3 and R5 are as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridinonetriazine Derivative, and methods of using the 4-Pyridinonetriazine Derivatives for treating or preventing HIV infection in a subject.

Syntheses of precursors and reference compounds of the melanin- concentrating hormone receptor 1 (MCHR1) Tracers [11C]SNAP-7941 and [18F]FE@SNAP for positron emission tomography

The MCH receptor has been revealed as a target of great interest in positron emission tomography imaging. The receptor's eponymous substrate melanin-concentrating hormone (MCH) is a cyclic peptide hormone, which is located predominantly in the hypothalamus with a major influence on energy and weight regulation as well as water balance and memory. Therefore, it is thought to play an important role in the pathophysiology of adiposity, which is nowadays a big issue worldwide. Based on the selective and high-affinity MCH receptor 1 antagonist SNAP-7941, a series of novel SNAP derivatives has been developed to provide different precursors and reference compounds for the radiosyntheses of the novel PET radiotracers [11C]SNAP-7941 and [18F] FE@SNAP. Positron emission tomography promotes a better understanding of physiologic parameters on a molecular level, thus giving a deeper insight into MCHR1 related processes as adiposity.

Biomimetic synthesis, antibacterial activity and structure-activity properties of the pyroglutamate core of oxazolomycin

Biomimetic intramolecular aldol reactions on oxazolidine templates derived from serine may be used to generate densely functionalised pyroglutamates, which are simpler mimics of the right hand side of oxazolomycin. Some of the compounds from this sequence exhibit in vivo activity against S. aureus and E. coli, suggesting that pyroglutamate scaffolds may be useful templates for the development of novel antibacterials, and cheminformatic analysis has been used to provide some structure-activity data.

Dihydropyrazolopyrimidines containing benzimidazoles as KV1.5 potassium channel antagonists

Dihydropyrazolopyrimidines with a C6 heterocycle substituent were found to have high potency for block of KV1.5. Investigation of the substitution in the benzimidazole ring and the substituent in the 5-position of the dihydropyrazolopyrimidine

A novel, efficient, diastereo- and enantioselective mukaiyama aldol-based synthesis of a vinyl cyclopentanone core derivative of viridenomycin

A strategy has been developed for a rapid seven-step construction of a chiral, nonracemic vinyl cyclopentanone building block as part of a synthetic approach to viridenomycin, using a diastereo- and enantioselective Mukaiyama aldol and intramolecular Knoe

PYRROLOPYRIDAZINE DERIVATIVES

The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-α mediated diseases.