90741-33-6

Upstream product

• 90741-31-4 (S)-N-benzyl-5-thioxoproline tert-butyl ester 
• 96-32-2 bromoacetic acid methyl ester 
• 90741-27-8 (S)-tert-butyl 1-benzyl-5-oxopyrrolidine-2-carboxylate 
• 56-86-0 L-glutamic acid 
• 100-52-7 benzaldehyde 
• 77539-18-5 (S)-(+)-2-benzylamino glutaric acid 
• 38854-94-3 N-benzyl-L-pyroglutamic acid 
• 16695-14-0 Malonic acid monomethyl ester 

Downstream Products

• 182137-24-2 (2S,5R)-1-(benzyloxycarbonyl)-5-[(methoxycarbonyl)methyl]proline tert-butyl ester 
• 90741-36-9 (2R-cis)-5-((1,1-Dimethylethoxy)carbonyl)-1-(phenylmethyl)-2-pyrrolidineacetic acid methyl ester 
• 182266-46-2 (2S,5R)-5-((R)-2-Bromo-1-triethylsilanyloxy-ethyl)-pyrrolidine-1,2-dicarboxylic acid 1-benzyl ester 2-tert-butyl ester 
• 182137-73-1 (2S,5R)-5-((S)-2-Bromo-1-triethylsilanyloxy-ethyl)-pyrrolidine-1,2-dicarboxylic acid 1-benzyl ester 2-tert-butyl ester 
• 182137-71-9 (2S,5R)-(S)-5-Oxiranyl-pyrrolidine-1,2-dicarboxylic acid 1-benzyl ester 2-tert-butyl ester 
• 182266-45-1 (2S,5R)-(R)-5-Oxiranyl-pyrrolidine-1,2-dicarboxylic acid 1-benzyl ester 2-tert-butyl ester 
• 182138-57-4 (1S,3S,4R)-3-Triethylsilanyloxy-7-aza-bicyclo[2.2.1]heptane-1,7-dicarboxylic acid 7-benzyl ester 1-tert-butyl ester 
• 182137-68-4 (2S,5R)-5-(2-Methanesulfonyloxy-ethyl)-pyrrolidine-1,2-dicarboxylic acid 1-benzyl ester 2-tert-butyl ester 
• 182137-69-5 (2S,5R)-5-(2-Phenylselanyl-ethyl)-pyrrolidine-1,2-dicarboxylic acid 1-benzyl ester 2-tert-butyl ester 
• 178813-40-6 (2S,5R)-5-(2-Hydroxy-ethyl)-pyrrolidine-1,2-dicarboxylic acid 1-benzyl ester 2-tert-butyl ester 
• 182137-38-8 (2S,5R)-5-(2-Bromo-ethyl)-pyrrolidine-1,2-dicarboxylic acid 1-benzyl ester 2-tert-butyl ester 
• 90741-40-5 tert-butyl (2R,5R)-1-benzyl-5-(2-hydroxyethyl)pyrrolidine-2-carboxylate 
• 113472-56-3 (2S)-cis-1-(benzyloxycarbonyl)-5-vinylproline tert-butyl ester 

Relevant academic research and scientific papers

A Direct, Versatile, and Chemoselective Synthesis of Vinylogous Bis- and Monourethanes/amides and β-Keto Esters by Aza-Knoevenagel-Type Reactions of Tertiary Amides with Enolates

Full details of our investigations into aza-Knoevenagel-type reactions with common tertiary amides as the electrophilic partner are reported. The method is based on the addition of stabilized carbanionic nucleophiles to the amides, which are activated in situ with triflic anhydride (Tf2O). The reaction proceeds under mild conditions and tolerates several sensitive functional groups including enamide and tert-butyldimethylsilyloxy (TBSO) groups. Significantly, with amides bearing more reactive ester, cyano, and aldehyde groups, the reaction occurs chemoselectively at the least reactive amide group. Such “umpolung” of the chemoselectivity in C=C bond formation is challenging, rare, and of synthetic value. Vinylogous bis-urethanes (aza-Knoevenagel-type condensation products), vinylogous urethanes, and vinylogous amides can be synthesized by employing enolates/carbanions generated from methyl ketones, malonic acid monoester, 2-phenylacetate, or (benzylsulfonyl)benzene. Moreover, when higher homologues of acetate were used, β-keto esters were obtained directly from amides. The method has been applied to the one-step syntheses of several known key intermediates in the total syntheses of alkaloids and 4-quinolone antibiotics. An efficient and mild intramolecular Friedel–Crafts-type cyclization of an anilinyl ester has also been achieved with Tf2O as an effective promoter. This amide-based method is a direct and umpoled alternative to the versatile but stepwise one based on thionation and the Eschenmoser sulfide contraction.

A the non-peptide class perishes weakly inhibiting protein antagonists and its synthetic method and application (by machine translation)

This invention discloses a kind of the non-peptide class perishes weakly inhibiting protein antagonist and method for preparing the same and application, which aims to provide a better anticancer effect with the non-peptide class perishes weakly inhibitin

Inhibitors of α4β1 mediated cell adhesion

The present invention relates to compound of formula (I), that are potent inhibitors of α4β1mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of inflammatory diseases. Specifically, the molecules of the present invention can be used for treating or preventing α4β1adhesion mediated conditions in a mammal such as a human. This method may comprise administering to a mammal or a human patient an effective amount of the compound or composition as explained in the present specification.

Chirospecific synthesis of conformationally constrained 7-azabicycloheptane amino acids by transannular alkylation

A new method is reported for the chirospecific preparation of optically pure 1-carboxy-7-azabicycloheptane amino acids for the generation of peptidomimetics as conformational probes. The method allows for the multigram preparation of these amino acid analogues through use of a thiolactam sulfide contraction and a transannular alkylation sequence as the key C-C bond-forming steps, starting from L-glutamic acid. The route provides access to two common intermediates, 7-(benzyloxycarbonyl)-1-carboxy-7-azabicyclo[2.2.1]-3-heptane and (1S,4R)-7-(benzyloxycarbonyl)-1-carboxy-7-azabicyclo[2.2.1]-3-heptanon e tert-butyl ester, for elaboration to symmetrical and chiral amino acid homologues, respectively. Decarboxylation of the C-1 carboxy unit of the latter intermediate also demonstrated the applicability of the method for a short, chirospecific preparation of a (+)-epibatidine intermediate, (1S,4R)-7-(tert-butyloxycarbonyl)-1-carboxy-7-azabicyclo[2.2.1]3-hepta none.