82961-76-0

Upstream product

• 17790-81-7 methyl 4-bromo-3-oxobutanoate 
• 100-51-6 benzyl alcohol 
• 32807-28-6 Methyl 4-chloroacetoacetate 
• 19810-31-2 Benzyloxyacetyl chloride 
• 30379-55-6 benzyloxyacetic acid 
• 67-56-1 methanol 
• 82961-71-5 5-(2-Benzyloxy-1-hydroxy-ethylidene)-2,2-dimethyl-[1,3]dioxane-4,6-dione 

Downstream Products

• 415678-68-1 (2,4-dimethyl-3-pentyl) γ-benzyloxyacetoacetate 
• 1206102-11-5 (4R,12aS)-7-(benzyloxy)-N-(2,4-difluorobenzyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1′,2’:4,5]-pyrazino[2,1-b][1,3]oxazine-9-carboxamide 
• 1229006-21-6 1-[2,2-bis(methyloxy)ethyl]-5-({[(2,4-difluorophenyl)methyl]amino}carbonyl)-4-oxo-3-[(phenylmethyl)oxy]-1,4-dihydro-2-pyridinecarboxylic acid methyl ester 
• 1357289-08-7 2,5-dimethyl 3-(benzyloxy)-1-(2,2-dimethoxyethyl)-4-oxo-1,4-dihydropyridine-2,5-dicarboxylate 
• 1357289-10-1 C₂₁H₂₂N₂O₆ 
• 1246617-67-3 C₁₈H₁₇NO₇ 
• 1229006-25-0 methyl 3-(benzyloxy)-5-(2,4-difluorobenzylcarbamoyl)-4-oxo-1-(2-oxoethyl)-1,4-dihydropyridine-2-carboxylate 
• 1357289-24-7 C₂₈H₂₉F₂N₃O₆ 
• 1357289-26-9 C₂₇H₂₇F₂N₃O₆ 
• 1357289-27-0 C₂₇H₂₅F₂N₃O₅ 
• 99788-90-6 (E,Z)-4-Benzyloxy-2-methoxymethylen-3-oxobuttersaeure-methylester 
• 119736-16-2 3-(benzyloxy)-1-((tert-butoxycarbonyl)amino)-4-oxo-1,4-dihydropyridine-2-carboxylic acid ethyl ester 
• 114784-19-9 (R)-Methyl 4-benzyloxy-3-hydroxybutanoate 
• 147849-60-3 Methyl (S)-4-(benzyloxy)-3-hydroxybutanoate 

Relevant academic research and scientific papers

Synthesis method of 3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylic acid

The invention discloses a synthesis method of 3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylic acid. The synthesis method sequentially comprises the following steps: S1, condensing 4-chloroacetoacetate and benzyl alcohol to obtain an intermediate I; S2, condensing the intermediate I with N,N-dimethylformamide dimethyl acetal to obtain an intermediate II; S3, performing ring closing on the intermediate IIand oxalic acid diester to obtain an intermediate III; and S4, decarboxylating the intermediate III in an acidic aqueous solution to obtain a target product. The method has the advantages of simple steps, mild conditions, cheap and easily available raw materials, and reduction of the cost of a target patent medicine.

Practical Synthetic Method for the Preparation of Pyrone Diesters: An Efficient Synthetic Route for the Synthesis of Dolutegravir Sodium

A highly efficient and practical synthetic method for the preparation of pyrone diesters was established. The pyrone diester 3c can be prepared from readily available starting materials on a multihundred gram scale. The pyrone diester 3c can easily be converted to dolutegravir sodium (1). The synthetic route demonstrated herein provides an efficient and atom-economical synthetic method for preparing this potent anti-HIV agent.

Method for synthesizing diastereomer impurity in dolutegravir raw material

The invention provides a method for synthesizing a diastereomer impurity in a dolutegravir raw material, which comprises the following steps: 1, carrying out condensation reaction on SM1 serving as araw material and 2,4-difluorobenzylamine to generate a compound I; 2, reacting the compound I with an alkali in a reaction solvent to generate a compound II; 3, hydrolyzing the compound II under an acidic condition to generate a compound III; 4, carrying out acid catalytic reaction on the compound III and R-aminobutanol in a reaction solvent to generate a compound IV; 5, generating a compound V from the compound IV in a reaction solvent under the catalysis of a condensing agent; and 6, demethylating the compound V under the action of an alkali metal salt to generate an impurity VI. The synthetic method of the diastereoisomer impurity in the dolutegravir raw material is simple in process and available in raw material, and the prepared new impurity can provide a reference substance for quality analysis of dolutegravir, so that the quality standard of dolutegravir is improved.

NEW ANALOGS AS ANDROGEN RECEPTOR AND GLUCOCORTICOID RECEPTOR MODULATORS

The present invention relates to novel dihydropyridine derivatives of formula (I): as modulators of nuclear receptors selected from androgen receptor and glucocorticoid receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by modulation of androgen receptor and/or glucocorticoid receptor, selected from cancer, metastasizing cancers, benign prostate hyperplasia, polycystic ovary syndrome (PCOS), hair loss, hirsutism, acne, hypogonadism, muscle wasting diseases, cachexia, Cushing's syndrome, anti-psychotic drug induced weight gain, obesity, post-traumatic stress disorder and alcoholism.

Synthesis method of dolutegravir intermediate, and related substance detection method thereof

The invention discloses a synthesis method of a dolutegravir intermediate, and a related substance detection method thereof. 4-chloroacetoacetic acid methyl ester and phenylcarbinol are adopted as starting materials, and the dolutegravir intermediate i is obtained through four steps of reaction; the reaction conditions are simple, only methylbenzene is used as a solvent in reaction, the raw materials are easy to get, the obtained product is treated and purified through column chromatography, the yield of the product obtained by each step reaches up to 90 percent or above, and the synthesis method is suitable for industrial production; the related substance detection method of the dolutegravir intermediate i adopts high performance liquid chromatography; through testing, the content of thedolutegravir intermediate i related substance is 99.6 percent, the separation degree of each impurity is larger than 3.0, and the separation degree is better.

PROCESS FOR PREPARING COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY

A process for preparing a compound represented by formula (Y1) or (Y2) [wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R1d is hydrogen, halogen, or the like; R2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R4d is a lower alkyl optionally substituted with substituent E, or the like; and R6d is a lower alkyl group optionally substituted with substituent group E, or the like].

7-HYDROXY-PYRAZOLO[1,5-A] PYRIMIDINE COMPOUNDS AND THEIR USE AS CCR2 RECEPTOR ANTAGONISTS

The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R1-7 and A are as defined in the claims.

METHOD OF PRODUCING PYRONE AND PYRIDONE DERIVATIVES

The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.

7-HYDROXY-PYRAZOLO[1,5-A] PYRIMIDINE COMPOUNDS AND THEIR USE AS CCR2 RECEPTOR ANTAGONISTS

The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R1-7 and A are as defined in the claims.

PYRROLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

The subject of the invention is compounds of formula (I): in which R1-R10 are as defined within, the method of preparation and therapeutic application as cannabinoid CB 1 receptor antagonists