54384-05-3

Upstream product

• 107-97-1 sarcosine 
• 100-51-6 benzyl alcohol 
• 87746-58-5 benzyl 2-((tert-butoxycarbonyl)methylamino)acetate 

Downstream Products

• 148205-67-8 Z(OMe)-Arg(NO₂)-Sar-OBzl 
• 1204215-19-9 C₂₅H₃₂N₂O₅ 
• 1620161-93-4 (6S,9S)-benzyl 6,9-dibenzyl-2,2,14-trimethyl-4,7,10,13-tetraoxo-3-oxa-5,8,11,14-tetraazahexadecan-16-oate 
• 1092972-80-9 C₂₂H₃₁NO₇ 
• 1353658-26-0 Benzyl 2-((6R,6aS,14aR)-1,6,8,14a-tetrahydroxy-11-((3R,4R,5R,6S)-4-hydroxy-3,5-dimethoxy-6-methyltetrahydro-2H-pyran-2-ylamino)-6a-methoxy-N,3-dimethyl-7,9,12,14-tetraoxo-5,6,6a,7,9,12,14,14a-octahydrobenzo[a]tetracene-2-carboxamido)acetate 

Relevant academic research and scientific papers

RAS INHIBITORS

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

Bioorthogonal release of anticancer drugs: Via gold-triggered 2-alkynylbenzamide cyclization

Metal-based uncaging of biomolecules has become an emerging approach for in vivo applications, which is largely due to the advantageous bioorthogonality of abiotic transition metals. Adding to the library of metal-cleavable protecting groups, this work introduces the 2-alkynylbenzamide (Ayba) moiety for the gold-triggered release of secondary amines under mild and physiological conditions. Studies were further performed to highlight some intrinsic benefits of the Ayba protecting group, which are (1) its amenable nature to derivatization for manipulating prodrug properties, and (2) its orthogonality with other commonly used transition metals like palladium and ruthenium. With a focus on highlighting its application for anticancer drug therapies, this study successfully shows that gold-triggered conversion of Ayba-protected prodrugs into bioactive anticancer drugs (i.e. doxorubicin, endoxifen) can proceed effectively in cell-based assays.

DRUGS TO TREAT OCULAR DISORDERS

The present invention provides new prodrugs of therapeutically active loop diuretics, including oligomeric prodrugs, and compositions to treat medical disorders, for example, ocular disorders such as glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

Zinc-acetic acid promoted reductive carbon-nitrogen bond cleavage reaction of α-aminoketones

Scope and limitation of the reductive cleavage reaction of α-aminoketone systems with zinc-acetic acid are described. The carbon-nitrogen bond cleavage reaction was applicable to a wide range of α-aminoalkyl aryl ketones possessing various substituents on the aromatic ring. In contrast, α-aminoalkyl alkyl ketones with protons at the α'-position or α-aminoesters were sluggish to the carbon-nitrogen cleavage reaction.

Synthesis of palau'amide and its diastereomers: confirmation of its stereostructure

Four diastereomers of palau'amide (1-4), a cytotoxic cyclodepsipeptide, were synthesized. The 1H NMR spectrum of 1 was identical to that of natural palau'amide. This established the complete stereostructure of palau'amide.