110207-94-8

Upstream product

• 53097-35-1 3-(prop-1-en-2-yl)benzonitrile 
• 6136-68-1 3-acethylbenzonitrile 
• 618-45-1 3-isopropylhydroxybenzene 
• 80841-09-4 meta-isopropylphenol trifluoromethanesulfonate 
• 1385069-08-8 C₁₅H₂₃NO₂ 
• 40751-59-5 3-isopropyl benzonitrile 

Downstream Products

• 850426-66-3 tert-butyl ((2S,3R)-3-hydroxy-4-((3-isopropylbenzyl)amino)-1-phenylbutan-2-yl)carbamate 
• 900800-08-0 [(1S,2R)-1-(3-allyl-benzyl)-2-hydroxy-3-(3-isopropyl-benzylamino)-propyl]-carbamic acid tert-butyl ester 
• 900798-38-1 (S)-4-[(R)-1-hydroxy-2-(3-isopropylbenzylamino)ethyl]-2-oxo-11,16-dioxa-3-azatricyclo[15.3.1.1*6,10*]docosa-1⁽²¹⁾,6,8,10⁽²²⁾,17,19-hexaene-19-carboxylic acid dimethylamide 
• 1385068-13-2 N-((E)-(4S,11R)-4-[(R)-1-hydroxy-2-(3-isopropyl-benzylamino)-ethyl]-2,13-dioxo-11-phenyl-6-oxa-3,12-diaza-bicyclo[12.3.1]octadeca-1⁽¹⁸⁾,8,14,16-tetraen-16-yl)-N-methyl-methanesulfonamide 
• 1385068-24-5 (E)-(4S,11S)-4-[(R)-1-hydroxy-2-(3-isopropyl-benzylamino)-ethyl]-16-methyl-11-phenyl-6-oxa-3,12-diaza-bicyclo[12.3.1]octadeca-1⁽¹⁸⁾,8,14,16-tetraene-2,13-dione 
• 1385068-28-9 (E)-(4S,11R)-4-[(R)-1-hydroxy-2-(3-isopropyl-benzylamino)-ethyl]-16-methyl-11-phenyl-6-oxa-3,12-diaza-bicyclo[12.3.1]octadeca-1⁽¹⁸⁾,8,14,16-tetraene-2,13-dione 
• 1385068-20-1 (E)-(S)-4-[(R)-1-hydroxy-2-(3-isopropyl-benzylamino)-ethyl]-16-methyl-6-oxa-3,12-diaza-bicyclo[12.3.1]octadeca-1⁽¹⁸⁾,8,14,16-tetraene-2,13-dione 
• 1385067-96-8 N-((S)-4-[(R)-1-hydroxy-2-(3-isopropyl-benzylamino)-ethyl]-2,13-dioxo-6-oxa-3,12-diaza-bicyclo[12.3.1]octadeca-1⁽¹⁸⁾,14,16-trien-16-yl)-N-methyl-methanesulfonamide 
• 1385067-85-5 N-((E)-(S)-4-[(R)-1-hydroxy-2-(3-isopropyl-benzylamino)-ethyl]-2,14-dioxo-6-oxa-3,13-diaza-bicyclo[13.3.1]nonadeca-1⁽¹⁸⁾,8,15⁽¹⁹⁾,16-tetraen-17-yl)-N-methyl-methanesulfonamide 
• 1385068-01-8 N-((S)-4-[(R)-1-hydroxy-2-(3-isopropyl-benzylamino)-ethyl]-2,14-dioxo-6-oxa-3,13-diaza-bicyclo[13.3.1]nonadeca-1⁽¹⁹⁾,15,17-trien-17-yl)-N-methyl-methanesulfonamide 
• 1385067-68-4 N-((E)-(S)-4-[(R)-1-hydroxy-2-(3-isopropyl-benzylamino)-ethyl]-2,13-dioxo-6-oxa-3,12-diaza-bicyclo[12.3.1]octadeca-1⁽¹⁸⁾,8,14,16-tetraen-16-yl)-N-methyl-methanesulfonamide 
• 1385068-07-4 N-((Z)-(S)-4-[(R)-1-hydroxy-2-(3-isopropyl-benzylamino)-ethyl]-12-methyl-2,13-dioxo-6-oxa-3,12-diaza-bicyclo[12.3.1]octadeca-1⁽¹⁸⁾,8,14,16-tetraen-16-yl)-N-methyl-methanesulfonamide 
• 1385068-10-9 N-((E)-(4S,11S)-4-[(R)-1-hydroxy-2-(3-isopropyl-benzylamino)-ethyl]-2,13-dioxo-11-phenyl-6-oxa-3,12-diaza-bicyclo[12.3.1]octadeca-1⁽¹⁸⁾,8,14,16-tetraen-16-yl)-N-methyl-methanesulfonamide 

Relevant academic research and scientific papers

Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core: Design, synthesis and X-ray crystal structures of enzyme inhibitor complexes

A series of P1-P3 linked macrocyclic BACE-1 inhibitors containing a hydroxyethylamine (HEA) isostere scaffold has been synthesized. All inhibitors comprise a toluene or N-phenylmethanesulfonamide P2 moiety. Excellent BACE-1 potencies, both in enzymatic an

COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF

The present invention provides novel beta-secretase inhibitors of the general formula (I), where the variables A1, A2, L1, L2, L3, R1, R2, R3, R4, R5, R6 and R7 are as defined in the claims, a method for their use in treating Alzheimer's disease, and methods for their use in reducing memapsin 2 catalytic activity.