89536-99-2

Upstream product

• 53363-89-6 N-t-butoxycarbonyl-N-methyl-L-leucine 
• 16652-76-9 L-valine benzyl ester p-toluenesulfonate salt 
• 100-52-7 benzaldehyde 
• 1356155-99-1 Boc-MeLeu-SH 
• 799779-66-1 (S)-2-Isocyano-3-methyl-butyric acid benzyl ester 
• 13139-15-6 N-tert-butoxycarbonyl-L-leucine 
• 89536-89-0 benzyl (2S)-3-methyl-2-(methylamino)butanoate hydrochloride 
• 109745-93-9 N-Benzyliden-(S)-valin-benzylester 
• 81135-38-8 benzyl (2S)-3-methyl-2-(methylamino)butanoate 
• 45170-31-8 Boc-N-Me-Val-OH 
• 109745-82-6 (S)-2-[(3-Cyano-4,6-dimethyl-pyridin-2-ylsulfanyl)-methyl-amino]-3-methyl-butyric acid benzyl ester 

Downstream Products

• 89537-08-6 Boc-MeLeu-MeLeu-MeVal-OBzl 

Relevant academic research and scientific papers

DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS

The present invention concerns a compound of following formula (I): where: - R1 is H or OH, - R2 is a (C1-C6)alkyl, COOH, COO-((C1-C6)alkyl) or thiazolyl group, - R3 is H or a (C1-C6)alkyl group, and - R4 is: ■ a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR5R6, ■ -(CH2CH2X1)(CH2CH2X2)a2(CH2CH2X3)a3(CH2CH2X4)a4(CH2CH2X5)a5R7, ■ an aryl-(C1-C8)alkyl group substituted by one or more groups chosen from among OH and NR9R10 groups, or ■ a heterocycle-(C1-C8)alkyl group optionally substituted by one or more groups chosen from among (C1-C6)alkyl, OH and NR12R13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.

Expanding the limits of isonitrile-mediated amidations: On the remarkable stereosubtleties of macrolactam formation from synthetic seco -cyclosporins

The scope of isonitrile-mediated amide bond-forming reactions is further explored in this second-generation synthetic approach to cyclosporine (cyclosporin A). Both type I and type II amidations are utilized in this effort, allowing access to epimeric cyclosporins A and H from a single precursor by variation of the coupling reagents. This work lends deeper insight into the relative acylating ability of the formimidate carboxylate mixed anhydride (FCMA) intermediate, while shedding light on the far-reaching impact of remote stereochemical changes on the effective preorganization of seco-cyclosporins.

Amino Acids and Peptides, 63. - Peptide Synthesis via N- or O-Activation of Amino Acids with 1,2-Dihydro-4,6-dimethyl-2-thioxo-3-pyridinecarbonitrile. - Synthesis of the 8-11 Tetrapeptide Sequence of Cyclosporin

Peptides and N-methyl peptides have been prepared in high yields and nearly free of racemisation via N-activation (Scheme 1) or O-activation (Scheme 2) of N-acylamino acids and N-acyl-N-methylamino acids, respectively, by 1,2-dihydro-4,6-dimethyl-2-thioxo