354153-36-9

Upstream product

• 354153-38-1 (S)-but-3-enyl[1-(tert-butyldiphenylsilanyloxymethyl)allyl]carbamic acid tert-butyl ester 
• 354153-37-0 1,1-dimethylethyl [(1S)-1-({[(1,1-dimethylethyl)(diphenyl)silyl]oxy}methyl)prop-2-en-1-yl]carbamate 
• 410540-37-3 1-(tert-butyl-diphenyl-silanyloxymethyl)-allylamine 
• 58479-61-1 tert-butylchlorodiphenylsilane 

Downstream Products

• 354153-41-6 (1S,2R,6R)-2-(tert-butyldiphenylsilanyloxymethyl)-7-oxa-3-azabicyclo[4.1.0]heptane-3-carboxylic acid tert-butyl ester 
• 354153-40-5 (1R,2R,6S)-2-(tert-butyldiphenylsilanyloxymethyl)-7-oxa-3-azabicyclo[4.1.0]heptane-3-carboxylic acid tert-butyl ester 
• 354153-39-2 (2R,3R,4S)-2-(tert-butyldiphenylsilanyloxymethyl)-3,4-dihydroxypiperidine-1-carboxylic acid tert-butyl ester 
• 53185-12-9 D-fagomine 
• 475630-67-2 (2R,3S,4R)-2-(hydroxymethyl)piperidine-3,4-diol 
• 475630-67-2 3-epi-fagomine 
• 475630-67-2 (2R,3S,4S)-2-(hydroxymethyl)piperidine-3,4-diol 
• 354153-43-8 2-(tert-butyl-diphenyl-silanyloxymethyl)-3-hydroxy-piperidine-1-carboxylic acid tert-butyl ester 
• 354153-42-7 (2R,3S)-2-(tert-butyldiphenylsilanyloxymethyl)-3-hydroxypiperidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

MACROCYCLIC LRRK2 KINASE INHIBITORS

The present invention relates to novel macrocyclic compounds of formula (I) and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease.

Asymmetric synthesis of the four possible fagomine isomers

The asymmetric synthesis of fagomine and its congeners 1-4 has been achieved by catalytic ring-closing metathesis (RCM). The synthesis involved the construction of the piperidene-type chiral building block 5 followed by dihydroxylation, starting from the D-serine-derived Garner aldehyde 6.

Asymmetric synthesis of fagomine and its congeners

The total synthesis of fagomine and its congeners 1-3 has been achieved starting from D-serine-derived Garner aldehyde 5 by catalytic ring-closing metathesis (RCM) for the construction of the piperidine ring followed by dihydroxylation.