82689-14-3

Upstream product

• 97530-05-7 (S)-tert-butyl (3-(1H-indol-3-yl)-1-(methoxy(methyl)amino)-1-oxopropan-2-yl)carbamate 
• 133039-97-1 t-butoxycarbonyltryptophan fluoride 
• 160235-08-5 N-(tert-butoxycarbonyl)-L-tryptophan N,O-dimethylhydroxamide 
• 154-09-6 L-tryptophanol 
• 24424-99-5 di-tert-butyl dicarbonate 
• 141215-69-2 methyl (2S)-2-{[(tert-butoxy)carbonyl]amino}-3-(1H-indol-3-yl)propanoate 
• 175837-77-1 Boc-Trp-N-carboxyanhydride 
• 144599-81-5 [(S)-2-(3,5-Dimethyl-pyrazol-1-yl)-1-(1H-indol-3-ylmethyl)-2-oxo-ethyl]-carbamic acid tert-butyl ester 
• 64411-38-7 N²-<(tert-butoxy)carbonyl>-L-tryptophane phenyl ester 
• 110659-38-6 N-t-butoxycarbonyl-tryptophanol 
• 13139-14-5 Boc-Trp-OH 

Downstream Products

• 103934-57-2 (tert-butyloxycarbonyl)-L-tryptophyl-ψ(CH2NH)-L-leucine benzyl ester 
• 1257632-05-5 C₄₁H₄₇N₅O₆ 

Relevant academic research and scientific papers

CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF

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

COMPOSITION AND METHODS OF USE OF SMALL MOLECULES AS BINDING LIGANDS FOR THE MODULATION OF PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9(PCSK9) PROTEIN ACTIVITY

This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modul

Small molecule compositions for sexual dysfunction

Compounds of the general formula: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, and X are as defined. Further provided are methods for treatment of sexual dysfunction, including erectile dysfunction and female sexual dysfunction, and combination drugs and method of use thereof, including a compound of the invention and one or more second sexual dysfunction pharmaceutical agents.

Pseudosymmetry in azabicyclo[2.1.1]hexanes. A stereoselective construction of the bicyclic core of peduncularine

Intramolecular photocycloaddition of 41 or its equivalent leads to the formation of photoadduct 25. While retro-Mannich fragmentation of the "b" bond in 25 leads to the formation of 44 (via 43), with the incorrect relative stereochemistry for the synthesi

INHIBITORS OF AKT ACTIVITY

Invented are novel pyridine compounds, the use of such compounds as inhibitors of PKB/AKT kinase activity and in the treatment of cancer and arthritis.

Pharmaceutical compounds

The present invention provides a compound of formula (I) or a salt thereof as well as methods of making and using same.

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.

Synthesis of chiral vinylogous sulfonamidopeptides (vs-peptides)

Chiral vinylogous amino sulfonic acids (vs-amino acids) were synthesized starting from either L- or D-α-amino acids via N-Boc-α-amino aldehydes. Wittig-Horner reaction with methyl (or ethyl) diethylphosphoryl methanesulfonate and nBuLi gave the corresponding α,β-unsaturated sulfonates in high yield and complete (E) stereoselectivity. Cleavage of the methyl (ethyl) ester was effected by treatment of the sulfonates with nBu4NI in refluxing acetone. Treatment of the nBu4N+ sulfonate salts with SO2Cl2/PPh3/CH2Cl2 gave the corresponding sulfonyl chlorides as stable chromatographable compounds. The synthetic sequence proved successful not only starting from α-amino acids carrying unfunctionalized side-chains (Ala, Val, Phe, Leu, Pro), but also with functionalized α-amino acids (Ser, Tyr, Gln) provided that the side chains were suitably protected. The sulfonyl chlorides were coupled with the amine salts to give vs-dipeptides. Amine hydrochlorides were prepared from N-Boc derivatives by treatment with HCl in methanol or ethyl acetate. The process was further iterated to give vstripeptides and vs-tetrapeptides. The above procedure was also used to synthesize "mixed" peptides, which incorporate both proteinogenic α-amino acids and vs-amino acids. Proteinogenic α-amino acids were incorporated at both the C-terminal and the N-terminal position.

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

Preparation of N2-protected amino acid aldehydes via reduction of corresponding acid halides with lithium tris-(tert.butoxy)-aluminium hydride

N2-FMOC amino aldehydes, N2-BOC amino aldehydes and N2-Z amino aldehydes are readily preparable from N2-FMOC amino acid chlorides and N2-BOC and N2-Z amino acid fluorides respectively, by r