221121-45-5

Upstream product

• 37517-78-5 magnesium bis(3-ethoxy-3-oxopropanoate) 
• 6148-64-7 ethyl potassium malonate 
• 221121-34-2 (2,6-dichlorophenylacetyl)imidazolide 
• 6575-24-2 2-(2,6-dichlorophenyl)acetic acid 
• 623-73-4 diazoacetic acid ethyl ester 
• 7623-19-0 2-(2,6-dichlorophenyl)oxirane 
• 61875-53-4 2,6-dichlorophenylacetylchloride 
• 105-53-3 diethyl malonate 

Downstream Products

• 221121-64-8 C₁₁H₈Cl₂N₂OS 
• 1391001-13-0 methyl 3-amino-4-(2,6-dichlorophenyl)butanoate 
• 1391000-98-8 2-(2,6-dichlorobenzyl)-4-{[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino}-1,6-naphthyridin-5(6H)-one trifluoroacetate 
• 1391001-32-3 2-(2,6-dichlorobenzyl)-4-chloro-1,6-naphthyridin-5⁽⁶⁾-one 
• 1391001-17-4 ethyl 6-(2,6-dichlorobenzyl)-4-chloro-2-methylpyridine-3-carboxylate 
• 1391001-16-3 ethyl 6-(2,6-dichlorobenzyl)-1,4-dihydro-2-methyl-4-oxopyridine-3-carboxylate 
• 1391001-15-2 ethyl 6-(2,6-dichlorobenzyl)-1,4,5,6-tetrahydro-2-methyl-4-oxopyridine-3-carboxylate 
• 1391001-14-1 ethyl 3-(1-(methoxycarbonyl)-3-(2,6-dichlorophenyl)propan-2-ylamino)but-2-enoate 
• 221121-64-8 6-(2,6-dichlorophenylmethyl)-3,4-dihydro-2-thiopyrimidin-4(3H)-one 

Relevant academic research and scientific papers

Synthesis and Biological Evaluation of a Series of 2-((1-substituted-1H-1,2,3-triazol-4-yl)methylthio)-6-(naphthalen-1-ylmethyl)pyrimidin-4(3H)-one As Potential HIV-1 Inhibitors

A series of novel S-DABO derivatives with the substituted 1,2,3-triazole moiety on the C-2 side chain were synthesized using the simple and efficient CuAAC reaction, and biologically evaluated as inhibitors of HIV-1. Among them, the most active HIV-1 inhi

Structural insight into the optimization of ethyl 5-hydroxybenzo[g]indol-3-carboxylates and their bioisosteric analogues as 5-LO/m-PGES-1 dual inhibitors able to suppress inflammation

The release of pro-inflammatory mediators, such as prostaglandines (PGs) and leukotrienes (LTs), arising from the arachidonic acid (AA) cascade, play a crucial role in initiating, maintaining, and regulating inflammatory processes. New dual inhibitors of 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1), that block, at the same time, the formation of PGE2 and LTs, are currently emerged as a highly interesting drug candidates for better pharmacotherapie of inflammation-related disorders. Following our previous studies, we here performed a detailed structure-based design of benzo[g]indol-3-carboxylate derivatives, disclosing several new key factors that affect both enzyme activity. Ethyl 2-(3,4-dichlorobenzyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate (4b, RAF-01) and ethyl 2-(3,4-dichlorophenyl)-5-hydroxy-1H-benzo[g]indole-3-carboxylate (7h, RAF-02) emerged as the most active compounds of the series. Additionally, together with selected structure based analogues, both derivatives displayed significant in vivo anti-inflammatory properties. In conclusion, modeling and experimental studies lead to the discovery of new candidate compounds prone to further developments as multi-target inhibitors of the inflammatory pathway.

Synthesis of aryl β-ketoesters by opening of aryl epoxides with ethyl diazoacetate catalyzed by BF3OEt2

A facile synthesis of 4-aryl substituted β-ketoesters from the reaction aryl epoxides with ethyl diazoacetate, in presence of BF 3OEt2 has been described with excellent yields.

BICYCLIC INHIBITORS OF ALK

The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R1, R2, R3, X, Y, Z, A, B, G1, m, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.

BICYCLIC INHIBITORS OF ANAPHASTIC LYMPHOMA KINASE

Disclosed are compounds of formula (Ⅰ) and their pharmaceutical acceptable salts, wherein R1, R2, R3, X, Y, Z, A, B, G1, m and n are defined in the description. The compositions containing the said compounds used for inhibiting kinases such as anaphastic lymphoma kinase (ALK) and methods of treating diseases such as cancer are disclosed.

BICYCLIC INHIBITORS OF ALK

The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R1, R2, R3, X, Y, Z, A, B, G1, m, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.

Synthesis and biological evaluation of novel 2-(substituted phenylaminocarbonylmethylthio)-6-(2,6-dichlorobenzyl)-pyrimidin-4(3H)-ones as potent HIV-1 NNRTIs

A series of novel 2-(phenylaminocarbonylmethylthio)-6-(2,6-dichlorobenzyl)-pyrimidin-4(3H)-ones have been designed and synthesized. All of the new compounds were evaluated for their anti-HIV activities in MT-4 cells. Most of these new compounds showed mod

5-alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure - Activity relationship profile

A series of dihydro-alkylthio-benzyl-oxopyrimidines (S-DABOs) bearing a 2-aryl-2-oxoethylsulfanyl chain at pyrimidine C2, an alkyl group at C5, and a 2,6-dichloro-, 2-chloro-6-fluoro-, and 2,6-difluoro-benzyl substitution at C6 (oxophenethyl-S-DABOs, 6-8)

Solution-phase parallel synthesis of S-DABO analogues

A simple and straightforward methodology for the parallel, solution-phase synthesis of a new series of S-DABO derivatives 1 and 2, bearing aromatic substituents at the C2 and C6 positions, has been developed. Starting from potassium ethyl malonates 3, thi

PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.