100129-12-2

Upstream product

• 22399-01-5 diethyl 2-(4-bromobenzylidene)malonate 
• 1353886-56-2 ethyl 3-(4-bromophenyl)-2-(hydroxyimino)propionate 
• 70146-78-0 diethyl 2-(4-bromobenzyl)malonate 
• 1122-91-4 4-bromo-benzaldehyde 
• 64-17-5 ethanol 
• 14091-15-7 p-bromo-DL-phenylalanine 

Downstream Products

• 140202-28-4 ethyl 4-bromo-N-acetylphenylalaninate 
• 1621399-56-1 N-(2-aminophenyl)-7-(piperazin-1-yl)isoquinoline-3-carboxamide 
• 1621399-75-4 tert-butyl 4-(3-(2-aminophenylcarbamoyl)-isoquinolin-7-yl)piperazine-1-carboxylate 
• 1621399-58-3 C₂₃H₂₄FN₅O 
• 1621399-78-7 tert-butyl 4-(3-(2-amino-4-fluorophenylcarbamoyl)-8-cyclopropylisoquinolin-7-yl)piperazine-1-carboxylate 
• 1621399-57-2 C₂₃H₂₅N₅O 
• 1621399-77-6 tert-butyl 4-(3-(2-aminophenylcarbamoyl)-8-cyclopropylisoquinolin-7-yl)piperazine-1-carboxylate 
• 660830-62-6 ethyl 7-bromoisoquinoline-3-carboxylate 

Relevant academic research and scientific papers

IMIDAZOPYRAZINE DERIVATIVES, PROCESS FOR PREPARATION THEREOF, AND THEIR USES AS LUCIFERINS

The present invention is in the field of bioluminescence in biology and/or medicine. In particular, the invention provides imidazopyrazine derivatives, processes for preparation thereof, and their uses as luciferins.

Unnatural α-amino ethyl esters from diethyl malonate or ethyl β-bromo-α-hydroxyiminocarboxylate

We have explored here the scope of the age-old diethyl malonate-based accesses to α-amino esters involving Knoevenagel condensations of diethyl malonate on aldehydes, reductions of the resulting alkylidenemalonates, the preparation of the corresponding α-hydroxyimino esters and their final reduction. This synthetic pathway turned out to be general although some unexpected limitations were encountered. The synthetic modifications of some of the intermediates - using Suzuki-Miyaura coupling or cycloadditions - before undertaking the oximation step - provided accesses to further α-amino esters. Moreover, other pathways to α-hydroxyimino esters were explored including an attempt to improve the cycloadditions between ethyl β-bromo-α-hydroxyiminocarboxylate and various alkylfuranes.

SELECTIVE HDAC1,2 INHIBITORS

Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.

HDAC1/2 INHIBITORS FOR THE TREATMENT OF NEURODEGENERATIVE AND/OR COGNITIVE DISORDERS

Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2.

Pd-catalyzed directed ortho -C-H alkenylation of phenylalanine derivatives

A practical Pd-catalyzed ortho-olefination of enantioenriched N-(SO2Py)-protected aryl-alanine and norephedrine derivatives with electron-deficient alkenes has been developed using N-fluoro-2,4,6-trimethylpyridinium triflate as the terminal oxidant. The reaction occurs efficiently with excellent monosubstitution selectivity and without loss of enantiopurity. This cross-coupling proved to be broad in scope, tolerating a variety of steric and electronic changes to both coupling partners. Removal of the directing group under mild conditions provides access to optically active tetrahydroisoquinoline-3-carboxylic acid derivatives (Tics) with good diastereocontrol and with very small erosion of enantiomeric purity.

SELECTIVE HDAC3 INHIBITORS

Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.

Iron-catalyzed oxidative C - H/C - H cross-coupling: An efficient route to α-quaternary α-amino acid derivatives

Fully loaded: A coordinating activation strategy has been developed to furnish α-quaternary α-amino acids through the iron(III)-catalyzed oxidative functionalization of α-C(sp3) - H bonds of α-tertiary α-amino acid esters. The reaction exhibits a broad substrate scope for both α-amino acids and nucleophiles (Nu) as well as good functional-group tolerance (see scheme, DTBP=di-tert-butyl peroxide, DCE=1,2-dichloroethane). Copyright

Resolution of N-protected amino acid esters using whole cells of Candida parapsilosis ATCC 7330

Whole cells of Candida parapsilosis ATCC 7330 were used for the resolution of N-acetyl amino acid esters. Excellent enantioselectivities (E = 40 to >500) were achieved for the resolution of N-protected protein and non-protein amino acid esters giving good yields (28-50%) and high enantiomeric excesses (up to >99%) for both enantiomers.