138754-84-4

Upstream product

• 24210-19-3 methyl (2S)-3-methyl-[(benzyloxy)carbonylamino]butanoate 
• 95500-74-6 N-Benzyloxycarbonyl-L-valinal diethylacetal 
• 6192-52-5 p-toluenesulfonic acid monohydrate 
• 861359-74-2 diisopropylethyl amine 
• 6216-65-5 N-benzyloxycarbonyl-L-valinol 
• 154674-66-5 (2S,5R,3E)-2-(Benzyloxymethoxy)-6-methyl-5-(benzyloxycarbonylamino)hept-3-ene 
• 260978-43-6 benzyl (1R)-1-(hydroxymethyl)-2-methylpropylcarbamate 
• 1149-26-4 (S)-N-(benzyloxycarbonyl)valine 
• 4467-55-4 N-Z-D-valine N-hydroxysuccinimide ester 
• 41445-88-9 (2-methylpropoxy)carbonyl N-[(benzyloxy)carbonyl]-D-valinate 
• 1685-33-2 N-[(benzyloxy)carbonyl]-D-valine 
• 2026-48-4 (S)-valinol 
• 501-53-1 benzyl chloroformate 
• 72-18-4 L-valine 

Downstream Products

• 109522-63-6 ethyl (4S)-4-(benzyloxycarbonyl)amino-2,2-difluoro-3-hydroxy-5-methylhexanoate 
• 6216-65-5 N-benzyloxycarbonyl-L-valinol 
• 137649-67-3 (3S,4R,5R,6S)-3,6-Bis-2,7-dimethyl-4,5-octanediol 
• 120629-95-0 3-<(benzyloxycarbonyl)amino>-2-hydroxy-4-methylpentanenitrile 
• 143914-86-7 (E)-(S)-4-Benzyloxycarbonylamino-2,5-dimethyl-hex-2-enoic acid ethyl ester 
• 796039-35-5 (4S)-4-benzyloxycarbonylamino-5-methylhex-2-enoic acid methyl ester 
• 848983-56-2 (E)-(S)-4-Benzyloxycarbonylamino-5-methyl-hex-2-enoic acid ethyl ester 
• 149357-26-6 (1S)-1-carbobenzyloxyamino-1-isopropyl-1-(4-methylimidazol-2-yl)methane 
• 95500-74-6 N-Benzyloxycarbonyl-L-valinal diethylacetal 
• 924627-10-1 ethyl (3R,4S)-4-{[(benzyloxy)carbonyl]amino}-3-hydroxy-5-methylhexanoate 
• 924627-07-6 ethyl (3S,4S)-4-{[(benzyloxy)carbonyl]amino}-3-hydroxy-5-methylhexanoate 

Relevant academic research and scientific papers

Discovery of (Dihydro)pyrazine N-Oxides via Genome Mining in Pseudomonas

Overexpression of the Pseudomonas virulence factor (pvf) biosynthetic operon led to the identification of a family of pyrazine N-oxides (PNOs), including a novel dihydropyrazine N,N′-dioxide (dPNO) metabolite. The nonribosomal peptide synthetase responsib

Synthesis of chiral branched allylamines through dual photoredox/nickel catalysis

Allylamines are versatile building blocks in the synthesis of various naturally occurring products and pharmaceuticals. In contrast to terminal allylamines, the methods of synthesis of their branched congeners with internal, stereodefined double bonds are less explored. This work describes a new approach for the preparation of allylaminesviacross-coupling of alkyl bromides with simple 3-bromoallylamines by merging the photoredox approach and Ni catalysis. The reaction proceeds under mild conditions, under blue light irradiation, and in the presence of an organic dye, 4CzIPN, as a photocatalyst. The scope of suitable reaction partners is broad, including alkyl bromides bearing reactive functionalities (e.g., esters, nitriles, aldehydes, ketones, epoxides) andN-protected allylamines, as well asN-allylated secondary and tertiary amines and heterocycles. The employment of non-racemic starting materials allows for rapid and easy construction of complex multifunctional allylamine derivatives without the loss of enantiomeric purity.

Synthetic method of key intermediate Tuv of natural anti-cancer drug Tubulysins

The invention belongs to the technical field of chemical synthesis, and particularly relates to a synthesis method of a key intermediate Tuv of a natural anti-cancer drug Tubulysins. With L-valinol (1) which is cheap and easy to obtain as a raw material,

Total synthesis of tubulysin U and N14-desacetoxytubulysin H

A concise and efficient procedure for the total synthesis of tubulysin U and N14-desacetoxytubulysin H has been developed with high stereoselectivity on a gram scale. This synthesis features an elegant cascade one-pot process to install the challenging th

Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity

Antibody-drug conjugates (ADCs) have become an important therapeutic modality for oncology, with three approved by the FDA and over 60 others in clinical trials. Despite the progress, improvements in ADC therapeutic index are desired. Peptide-based ADC linkers that are cleaved by lysosomal proteases have shown sufficient stability in serum and effective payload-release in targeted cells. If the linker can be preferentially hydrolyzed by tumor-specific proteases, safety margin may improve. However, the use of peptide-based linkers limits our ability to modulate protease specificity. Here we report the structure-guided discovery of novel, nonpeptidic ADC linkers. We show that a cyclobutane-1,1-dicarboxamide-containing linker is hydrolyzed predominantly by cathepsin B while the valine-citrulline dipeptide linker is not. ADCs bearing the nonpeptidic linker are as efficacious and stable in vivo as those with the dipeptide linker. Our results strongly support the application of the peptidomimetic linker and present new opportunities for improving the selectivity of ADCs.

FUMAGILLOL COMPOUNDS AND METHODS OF MAKING AND USING SAME

Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

ALIPHATIC PROLINAMIDE DERIVATIVES

This invention is directed to novel aliphatic prolinamide derivatives of Formula I, and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention. The compounds of the invention are inhibitors of HTRAl. Thus, the compounds of the invention are useful in the prevention and treatment of a wide range of diseases mediated (in whole or in part) by HTRAl. The compounds of the invention are also useful for inhibiting HTRAl protease activity in an eye or locus of an arthritis or related condition.

Chemoselective conversion from α-hydroxy acids to α-keto acids enabled by nitroxyl-radical-catalyzed aerobic oxidation

The chemoselective oxidation of α-hydroxy acids to α-keto acids catalyzed by 2-azaadamantane N-oxyl (AZADO), a nitroxyl radical catalyst, is described. Although α-keto acids are labile and can easily release CO2 under oxidation conditions, the use of molecular oxygen as a cooxidant enables the desired chemoselective oxidation.

PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF

This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.

PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF

This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.