637014-30-3

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 886370-56-5 (±)-trans-4-benzyl-1-(tert-butoxycarbonyl)pyrrolidine-3-carboxylic acid 
• 910095-61-3 C₁₂H₁₇NO 
• 122-78-1 phenylacetaldehyde 
• 54966-42-6 ethyl 3-benzylacrylate 
• 637014-20-1 (3R,4R,1'R)-3-benzyl-4-benzyloxymethyl-1-(1'-phenylethyl)pyrrolidin-2-one 
• 637014-26-7 (3R,4R,1'R)-3-benzyl-4-benzyloxymethyl-1-(1'-phenylethyl)-pyrrolidine 
• 637014-18-7 (4R,1'R)-4-benzyloxymethyl-1-(1'-phenylethyl)pyrrolidin-2-one 
• 190957-22-3 (4R,1'R)-1-(1'-phenylethyl)-4-hydroxymethylpyrrolidin-2-one 

Downstream Products

• 910050-01-0 ((3R,4R)-4-benzyl-pyrrolidin-3-yl)-methanol hydrochloride 
• 637014-31-4 methyl (3R,4R,)-4-benzyl-1-t-butoxycarbonyl-3-pyrrolidinecarboxylate 
• 886370-56-5 (3R,4R)-4-Benzyl-pyrrolidine-1,3-dicarboxylic acid 1-tert-butyl ester 

Relevant academic research and scientific papers

Diastereodivergent Access to Syn and Anti 3,4-Substituted β-Fluoropyrrolidines: Enhancing or Reversing Substrate Preference

A practical diastereodivergent access to β-fluoropyrrolidines with two adjacent stereocenters has been demonstrated, by either enhancing or completely reversing the substrate control, in the diastereoselective fluorination of a series of diverse pyrrolidi

The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches

The small-molecule trans-3,4-disubstituted pyrrolidine 6 was identified from in silico three-dimensional (3D) pharmacophore searches based on known X-ray structures of renin-inhibitor complexes and demonstrated to be a weakly active inhibitor of the human enzyme. The unexpected binding mode of the more potent enantiomer (3S,4S)-6a in an extended conformation spanning the nonprime and S1′ pockets of the recombinant human (rh)-renin active site was elucidated by X-ray crystallography. Initial structure-activity relationship work focused on modifications of the hydrophobic diphenylamine portion positioned in S1 and extending toward the S2 pocket. Replacement with an optimized P3-P1 pharmacophore interacting to the nonsubstrate S3sp cavity eventually resulted in significantly improved in vitro potency and selectivity. The prototype analogue (3S,4S)-12a of this new class of direct renin inhibitors exerted blood pressure lowering effects in a hypertensive double-transgenic rat model after oral administration.

PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS

Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on the activity of b

ORGANIC COMPOUNDS

Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel inter-mediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula (I), wherein the substituents are as described in the specificacion.

A stereoselective approach to both 3,4-trans-disubstituted pyrrolidin-2-ones and pyrrolidines. A convenient synthesis of (3R,4R)-4-benzyl-3-pyrrolidinecarboxylic acid

Chiral 4-alkyloxymethyl- and silyloxymethylpyrrolidin-2-ones, (10a-c), underwent alkylation to give the corresponding 3,4-trans-disubstituted pyrrolidin-2-ones, (11a-g), in good yield and total stereoselection, as shown by 1H NMR spectral data