138535-51-0

Upstream product

• 7517-19-3 methyl (L)-leucinate hydrochloride 
• 1939-99-7 benzenesulfonyl chloride 

Downstream Products

• 138535-48-5 (3S)-3<(1S)-N-benzylsulfonylamino-3-methylbutyl>-8-methoxy-3,4-dihydroisocoumarin 
• 663923-89-5 1-[N²,N³-bis(tert-butyloxycarbonyl)guanidino]-4-(N-phenylmethanesulfonyl-L-leucyl-L-prolyl-amino)butane 
• 663923-87-3 N-(phenylmethanesulfonyl)-L-leucyl-L-proline methyl ester 
• 663923-88-4 N-(phenylmethanesulfonyl)-L-leucyl-L-proline 
• 6297-57-0 (S)-4-methyl-2-(phenylmethylsulfonamido)pentanoic acid 
• 138535-41-8 N-benzylsulfonyl-(S)-leucinal 

Relevant academic research and scientific papers

New cyanopeptide-derived low molecular weight inhibitors of trypsin-like serine proteases

This paper deals with the design, syntheses, and inhibition tests of new low molecular weight thrombin inhibitors utilizing cyanopeptides, the secondary metabolites of cyanobacteria with interesting biological activities, as new lead structures. Starting with aeruginosin 98-B (1) as a lead structure, we have developed and synthesised new, selective acting inhibitors of serine proteases (RA-1005 and RA-1009), which are suitable targets for further structure-activity studies.

Efficient total synthesis of AI-77-B, a gastroprotective substance from Bacillus pumilus AI-77

First total synthesis of AI-77-B (1), a gastroprotective substance from Bacillus pumilus AI-77, was achieved in a stereoselective and convergent manner. In this synthesis, the dihydroisocoumarin part 2 was constructed in one step through 1,2-addition of the benzylic anion 17b to Boc-L-leucinal 7b. The hydroxy amino acid 4 was elaborated from (R)-glutamic acid in a highly stereoselective manner. Condensation of 2·HCl and 4, intramolecular Pinner reaction, followed by mild hydrolysis afforded AI-77-B (1).