50680-54-1

Upstream product

• 98070-84-9 dichloro-methoxy-acetic acid dimethylamide 
• 98486-39-6 ethoxy-dichloro-acetic acid dimethylamide 
• 79-37-8 oxalyl dichloride 
• 506-59-2 N,N-dimethylammonium chloride 
• 32833-96-8 N,N-dimethyloxamic acid 
• 124-40-3 dimethyl amine 

Downstream Products

• 519-65-3 Dimethylaminooxoessigsaeure-2-acetyl-2-methyl-1-phenylhydrazid 
• 99072-46-5 dimethyl-oxalamic acid-(4-nitro-phenyl ester) 
• 99060-43-2 dimethyl-oxalamic acid phenyl ester 
• 59571-38-9 methyl 2-(dimethylamino)-2-oxoacetate 
• 1039632-13-7 N-(N',N'-dimethyloxamoyl)-3-(S)-(1-(S)-phenylethyl)aminopyrrolidine 
• 1188426-10-9 N-ethyl-N-(2-((4-fluorobenzyl)carbamoyl)-3-hydroxy-4-oxo-6,7,8,9-tetrahydro-7,11-ethanopyrimido[1,2-a]azepin-10(4H)-yl)-N',N'-dimethylethanediamide 

Relevant academic research and scientific papers

Copper-Catalyzed Oxalamide-Directed ortho-C-H Amination of Anilines with Alkylamines

A copper-catalyzed oxalamide-directed ortho-C-H amination of anilines has been developed by using 1 atm of air as the sole oxidant. The protocol shows excellent functional group tolerance, and some heterocyclic amines including indole, benzothiophene, benzothiazole, quinoline, isoquinoline, and quinoxaline could be compatible in the reaction. The late-stage diversification of medicinal drugs demonstrates the synthetic utility of this protocol.

Synthesis of N-trifluoromethyl amides from carboxylic acids

Found in biomolecules, pharmaceuticals, and agrochemicals, amide-containing molecules are ubiquitous in nature, and their derivatization represents a significant methodological goal in fluorine chemistry. Trifluoromethyl amides have emerged as important functional groups frequently found in pharmaceutical compounds. To date, there is no strategy for synthesizing N-trifluoromethyl amides from abundant organic carboxylic acid derivatives, which are ideal starting materials in amide synthesis. Here, we report the synthesis of N-trifluoromethyl amides from carboxylic acid halides and esters under mild conditions via isothiocyanates in the presence of silver fluoride at room temperature. Through this strategy, isothiocyanates are desulfurized with AgF, and then the formed derivative is acylated to afford N-trifluoromethyl amides, including previously inaccessible structures. This method shows broad scope, provides a platform for rapidly generating N-trifluoromethyl amides by virtue of the diversity and availability of both reaction partners, and should find application in the modification of advanced intermediates.

Transformation of masked benzyl alcohols to: O -aminobenzaldehydes through C-H activation: A facile approach to quinazolines

Direct transformation of a directing group to important synthetic units would provide a high atom efficiency synthetic approach in synthetic chemistry. Herein, a convenient protocol for the synthesis of o-aminobenzaldehyde and benzoxazole derivatives from benzyl alcohols has been developed by employing (N,N-dimethyl)oxamoyl amide as a directing group in a palladium-catalyzed intramolecular amination. Furthermore, the attached directing center may not only be transformed into the product, but may also be further applied to generate synthetically important quinazoline and quinoline units. Finally, a high atom efficiency one-pot, two-step approach to form quinazolines from benzyl alcohol derivatives has been achieved in good yields, thus demonstrating its high utility.

HIV Integrase Inhibitors

The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

Kinase inhibitor compounds

The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.

Heterocyclic lithium amides as chiral ligands for an enantioselective hydroxyalkylation with n-BuLi

(Chemical Equation Presented) Chiral heterocyclic structures based on 3-aminopyrrolidines (3APs), 3-aminotetrahydrothiophens (3ATTs), and 3-aminotetrahydrofurans (3ATFs) have been synthesized. The corresponding lithium amides have been evaluated as chiral ligands in the condensation of n-BuLi on o-tolualdehyde. The returned levels of induction were in the 46-80% ee range. The cheap and easily prepared 3ATFLi's turned out to be also the best ligands, giving access to the expected R or S alcohols in a same 80% level of induction at -78°C in THF. In all cases, the sense of induction depends on the absolute configuration of C8 on the 3-amino appendage. A general concept is proposed to rationalize the process of induction in the presence of organolithium species.

KINASE INHIBITOR COMPOUNDS

The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.