97530-05-7

Upstream product

• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 13139-14-5 Boc-Trp-OH 
• 1117-97-1 N,0-dimethylhydroxylamine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 73-22-3 L-Tryptophan 

Downstream Products

• 195325-55-4 {(S)-1-(Methoxy-methyl-carbamoyl)-2-[1-(2,4,6-trimethyl-benzenesulfonyl)-1H-indol-3-yl]-ethyl}-carbamic acid tert-butyl ester 
• 97530-06-8 (tert-butyloxycarbonyl)-L-tryptophyl-ψ(CH2-NH)-L-leucyl-β-benzyl-L-aspartyl-L-phenylalanine amide 
• 97530-00-2 (tert-butyloxycarbonyl)-L-tryptophyl-ψ(CH2-NH)-L-leucyl-L-aspartyl-L-phenylalanine amide 
• 103934-57-2 (tert-butyloxycarbonyl)-L-tryptophyl-ψ(CH2NH)-L-leucine benzyl ester 
• 153828-80-9 5-<3,5-bis(trifluoromethyl)phenyl>-2-(N-Bocamino)-1-(3-indolyl)-3-pentanone 
• 157967-18-5 5-<3,5-bis(trifluoromethyl)phenyl>-2-(N-Bocamino)-1-(3-indolyl)-4-penten-3-one 
• 195325-57-6 (3S,4S)-4-tert-butyloxycarbonylamino-3-tetrahydropyranyloxy-5-3'-(N-mesitylene-2-sulfonyl)indolyl-1-pentene 
• 195325-71-4 (E)-(4R,5S)-5-tert-Butoxycarbonylamino-4-hydroxy-6-[1-(2,4,6-trimethyl-benzenesulfonyl)-1H-indol-3-yl]-hex-2-enoic acid methyl ester 
• 195325-56-5 (3S,4S)-4-tert-butyloxycarbonylamino-3-hydroxy-5-3'-(N-mesitylene-2-sulfonyl)indolyl-1-pentene 
• 195325-66-7 (3R,4S)-4-tert-butyloxycarbonylamino-3-hydroxy-5-3'-(N-mesitylene-2-sulfonyl)indolyl-1-pentene 

Relevant academic research and scientific papers

Isolation, structure elucidation, and total synthesis of tryptopeptins A and B, new TGF-?2 signaling modulators from streptomyces sp.

Two new microbial metabolites, tryptopeptins A (1) and B (2), were isolated from the cultured broth of Streptomyces sp. KUSC-G11, as modulators of the transforming growth factor-?2 (TGF-?2) signaling pathway. Their chemical structures consisting of isoval

Convenient Synthesis of Alternatively Bridged Tryptophan Ketopiperazines and Their Activities against Trypanosomatid Parasites

There is an urgent need for the development of new treatments against trypanosomatid parasites; the causative agents of some of the most debilitating diseases in the developing world. This work targets an interesting 6-5-6-6 fused carboline scaffold, accessing a range of substituted derivatives through stereospecific intramolecular Pictet–Spengler condensation. Modification of the cyclisation conditions allowed retention of the carbamate protecting group and gave insight into the reaction mechanism. Compounds’ bioactivities were measured against T. brucei, T. cruzi, L. major and HeLa cells. We have identified promising pan-trypanocidal lead compounds based on the core scaffold, and highlight key SAR trends which will be useful for the future development of these compounds as potent trypanocidal agents.

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.

CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF

Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

NOVEL COMPOUNDS

The invention provides compounds of general formula (I) or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are described throughout the description and claims. T

Preparation of Weinreb amides using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4- methylmorpholinium chloride (DMT-MM)

Weinreb amides were successfully prepared from the corresponding carboxylic acids using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride (DMT-MM) in the solvents, methanol, isopropyl alcohol, and acetonitrile, which can solubilize DMT-MM

Synthesis of new chiral peptide nucleic acid (PNA) monomers

We have synthesised a series of new chiral type I peptide nucleic acid monomers in total yields of 36-53%, derived from Val, Ile, Ser(Bzl), Pro, and Trp, employing convenient procedure.

A highly stereoselective synthesis of the functionalized (E)-alkene dipeptide isostere of Trp-Val via organocyanocopper-Lewis acid mediated reaction

A stereocontrolled synthesis of the (e)-alkene dipeptide isostere of Trp-Val is described. The stereospecific α-alkylation of the δ-amino-γ- mesyloxy-α,β-unsaturated ester via the organocyanocopper-Lewis acid mediated reaction, based on 1,3-transfer of ch

A convenient synthesis of N-methoxy-N-methylamides from carboxylic acids

Carboxylic acids can be converted to their corresponding N-methoxy-N-methylamides in high yields using 2-chloro-1-methylpyridinium iodide as the coupling agent. The reaction proceeds without racemization when chiral carboxylic acids are used as the starting material.

Tryptophan-derived NK1 antagonists: Conformationally constrained heterocyclic bioisosteres of the ester linkage

The 3,5-bis(trifluoromethyl)benzyl ester of N-acetyl-L-tryptophan 1 (L- 732,138) has been identified previously as a potent and selective substance P receptor antagonist. A series of analogs which introduced a 6-membered heterocyclic ring into the backbon