61274-13-3

Upstream product

• 6066-82-6 1-hydroxy-pyrrolidine-2,5-dione 
• 98-89-5 Cyclohexanecarboxylic acid 
• 2043-61-0 cyclohexanecarbaldehyde 

Downstream Products

• 1072896-46-8 p-methoxyphenyl (9-cyclohexanecarboxamido-3,5,9-trideoxy-5-glycolamido-D-glycero-α-D-galacto-2-nonulopyranosylonic acid)-(2->6)-β-D-galactopyranoside 
• 130340-71-5 N-(p-methylbenzyl)cyclohexanecarboxamide 
• 13810-02-1 N-hydroxycyclohexanecarboxamide 
• 1369515-43-4 N-((3-((3S,4S)-1-benzyl-4-methylpyrrolidin-3-yl)-5-oxo-4,5-dihydro-1,2,4-triazin-6-yl)methyl)tetrahydro-2H-pyran-4-carboxamide 
• 1000991-62-7 C₁₆H₂₁NO₄ 

Relevant academic research and scientific papers

Argininamide-type neuropeptide y Y1 receptor antagonists: The nature of: N Ω-carbamoyl substituents determines Y1R binding mode and affinity

The recently resolved crystal structure of the neuropeptide Y Y1 receptor (Y1R), co-crystallized with the high-affinity (pKi: 10.11), argininamide-type Y1R antagonist UR-MK299 (2), revealed that the NΩ-carbamoyl substituent (van der Waals volume: 139 ?3) is deeply buried in the receptor, occupying a hydrophobic pocket. We synthesized and characterized a series of argininamides, structurally related to 2. Y1R affinity decreased with increasing size of the carbamoyl residue (minimal pKi: 5.67). Exceeding a critical size of the substituent (van der Waals volume: 212 ?3), the ligands bound in an inverted mode with the carbamoyl side chain located at the surface of the receptor, as suggested by induced-fit docking and MD simulations.

New Class of Selective Estrogen Receptor Degraders (SERDs): Expanding the Toolbox of PROTAC Degrons

An effective endocrine therapy for breast cancer is to selectively and effectively degrade the estrogen receptor (ER). Up until now, there have been largely only two molecular scaffolds capable of doing this. In this study, we have developed new classes of scaffolds that possess selective estrogen receptor degrader (SERD) and ER antagonistic properties. These novel SERDs potently inhibit MCF-7 breast cancer cell proliferation and the expression of ER target genes, and their efficacy is comparable to Fulvestrant. Unlike Fulvestrant, the modular protein-targeted chimera (PROTAC)-type design of these novel SERDs should allow easy diversification into a library of analogs to further fine-tune their pharmacokinetic properties including oral availability. This work also expands the pool of currently available PROTAC-type scaffolds that could be beneficial for targeted degradation of various other therapeutically important proteins.

One-pot synthesis of hydroxamic acids from aldehydes and hydroxylamine

A one-pot oxidative transformation of aldehydes into hydroxamic acids by the use of an aqueous solution of hydroxylamine is reported. The methodology gives high yields and makes use of cheap, abundant and easily available reagents.

Aerobic amide bond formation with N-hydroxysuccinimide

Breathe easy: Molecular oxygen is one of the most abundant, atom-efficient, and economical oxidants. An aerobic oxidative amide formation from aldehydes and amines is reported. The method uses a catalytic amount of Co(OAc) 2 and N-hydroxysuccinimide as reaction promoters. It is applicable to chiral substrates without loss of their optical purity. Copyright

Convenient synthesis of N-hydroxysuccinimide esters from carboxylic acids using triphosgene

A simple and convenient method for the synthesis of N-hydroxysuccinimide ester is developed using triphosgene as an acid activator. Several aromatic and aliphatic N-hydroxysuccinimide esters are prepared from their corresponding carboxylic acids at room temperature in good yields in a rapid process using triphosgene. Some of the major advantages are mild conditions, good yields, and easy operation.