197891-68-2

Upstream product

• 1155374-00-7 4-(N-Boc-N-Z-amino)-1-butanol 
• 197891-66-0 4-benzyloxycarbamate-butyraldehyde diethyl acetal 
• 501-53-1 benzyl chloroformate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 197891-67-1 benzyloxycarbonyl-(4,4-diethoxy-butyl)-carbamic acid tert-butyl ester 

Downstream Products

• 197891-69-3 C₂₀H₂₇NO₇ 
• 1203455-23-5 C₂₄H₂₉NO₆S 
• 1421359-74-1 C₃₄H₅₀N₂O₁₃ 
• 197891-70-6 6-(Benzyloxycarbonyl-tert-butoxycarbonyl-amino)-4-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-hex-2E-enoic acid methyl ester 
• 197891-71-7 6-Benzyloxycarbonylamino-4-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-hex-2E-enoic acid methyl ester 
• 214050-58-5 (E)-6-Benzyloxycarbonylamino-4-(tert-butyl-dimethyl-silanyloxy)-hex-2-enoic acid methyl ester 
• 214050-57-4 (E)-6-Benzyloxycarbonylamino-4-hydroxy-hex-2-enoic acid methyl ester 

Relevant academic research and scientific papers

Dihydroxylation of vinyl sulfones: Stereoselective synthesis of (+)- and (-)-febrifugine and halofuginone

(Chemical Equation Presented) The asymmetric dihydroxylation of amino-functionalized vinyl sulfone 19 has been used for the 3-step preparation of 3-hydroxylpiperidine 24 in 86% enantiomeric excess. This enantiomerically enriched building block was used then to synthesize the naturally occurring antimalarial alkaloid febrifugine 1 and its antiangiogenic analogue, halofuginone 3.

Stereoselective syntheses of (E)-α,β-didehydroamino acid and peptide containing its residue utilizing oxazolidinone derivative

Reaction of methyl N-Boc-N-phenoxycarbonylglycinate with various aldehydes afforded the corresponding cis-4,5-oxazolidinone derivatives, which were effectively converted to (E)-α,β-didehydroamino acids by means of a base. Furthermore, N-deprotection of the oxazolidinone derivatives and subsequent coupling reaction with Boc-amino acid furnished the corresponding dipeptides, which were transformed to dipeptide containing α,α- didehydroamino acid with high E selectivity.

Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase

There are described according to the invention compounds of formula (I) (relative stereochemistry indicated), wherein R1, R2, R3 and X are as defined in the specification, together with processes for preparing them, compositions containing them and their use as pharmaceuticals. Compounds of formula (I) are indicated inter alia for the treatment of chronic bronchitis.