146398-01-8

Upstream product

• 71449-08-6 (2R)-2-{[(benzyloxy)carbonyl]amino}-4-tert-butoxy-4-oxobutanoic acid 

Downstream Products

• 1022975-13-8 (R)-4-oxo-3-{[(phenylmethoxy)carbonyl]amino}butanoic acid 1,1-dimethylethyl ester 
• 761435-74-9 (2R,3S)-2-(4-Hydroxy-benzenesulfonylmethyl)-pyrrolidine-3-carboxylic acid tert-butyl ester 
• 761435-57-8 (2R,3S)-2-(4-Hydroxy-benzenesulfonylmethyl)-piperidine-3-carboxylic acid tert-butyl ester 
• 761435-45-4 3-benzyloxycarbonylamino-4-(4-hydroxy-phenylsulfanyl)-butyric acid tert-butyl ester 
• 761435-76-1 (2R,3S)-2-(4-Hydroxy-benzenesulfonylmethyl)-pyrrolidine-1,3-dicarboxylic acid di-tert-butyl ester 
• 441298-09-5 (2R,3S)-2-(4-Hydroxy-benzenesulfonylmethyl)-piperidine-1,3-dicarboxylic acid di-tert-butyl ester 
• 761435-47-6 3-benzyloxycarbonylamino-4-(4-benzyloxy-phenylsulfanyl)-butyric acid tert-butyl ester 
• 761435-49-8 (S)-2-[(R)-1-Benzyloxycarbonylamino-2-(4-benzyloxy-phenylsulfanyl)-ethyl]-pent-4-enoic acid tert-butyl ester 
• 761435-72-7 (2S,3R)-4-(4-Benzyloxy-benzenesulfonyl)-3-benzyloxycarbonylamino-2-(2-oxo-ethyl)-butyric acid tert-butyl ester 
• 761435-55-6 (S)-2-[(R)-2-(4-Benzyloxy-benzenesulfonyl)-1-benzyloxycarbonylamino-ethyl]-5-oxo-pentanoic acid tert-butyl ester 
• 761435-51-2 (S)-2-[(R)-2-(4-Benzyloxy-benzenesulfonyl)-1-benzyloxycarbonylamino-ethyl]-pent-4-enoic acid tert-butyl ester 
• 441298-16-4 (2R,3S)-2-[4-(2-Methyl-quinolin-4-ylmethoxy)-benzenesulfonylmethyl]-pyrrolidine-1,3-dicarboxylic acid di-tert-butyl ester 
• 761435-53-4 (S)-2-[(R)-2-(4-Benzyloxy-benzenesulfonyl)-1-benzyloxycarbonylamino-ethyl]-5-hydroxy-pentanoic acid tert-butyl ester 
• 441298-10-8 (2R,3S)-2-[4-(2-Methyl-quinolin-4-ylmethoxy)-benzenesulfonylmethyl]-piperidine-1,3-dicarboxylic acid di-tert-butyl ester 

Relevant academic research and scientific papers

Synthesis method of (R)-tert-butyl 4-hydroxy-1-methoxybut-2-ylcarbamate

The invention belongs to the field of organic synthesis, and discloses a synthesis method of (R)-tert-butyl 4-hydroxy-1-methoxybut-2-ylcarbamate. The synthesis method disclosed by the invention comprises the following steps: (A) reacting a compound 1 with

Synthesis and structure-activity relationship of a novel sulfone series of TNF-α converting enzyme inhibitors

Replacement of the amide functionality in IM491 (N-hydroxy-(5S,6S)-1- methyl-6-{[4-(2-methyl-4-quinolinylmethoxy)anilinyl]carbonyl} -5-piperidinecarboxamide) with a sulfonyl group led to a new series of α,β-cyclic and β,β-cyclic γ-sulfonyl hydroxamic acids, which were potent TNF-α converting enzyme (TACE) inhibitors. Among them, inhibitor 4b (N-hydroxy-(4S,5S)-1-methyl-5-{[4-(2-methyl-4- quinolinylmethoxy)phenyl]sulfonylmethyl}-4-pyrrolidinecarboxamide) exhibited IC50 values of 1 nM and 180 nM in porcine TACE (pTACE) and cell assays, respectively, with excellent selectivity over MMP-1, -2, -9 and -13 and was orally bioavailable with an F value of 46% in mice.

Synthesis and evaluation of enantiomeric purity of protected α-amino and peptide aldehydes

The synthesis of enantiomerically pure Ac-Tyr-Val-Ala-Asp(O'Bu)-H dimethyl acetal ((S)-1) is reported, a protected tetrapeptide C-terminal aldehyde belonging to a class of potent, reversible inhibitors of cysteine proteases (e.g., interleukin-1β-convertin

Synthesis of enantiomerically pure β- and γ-amino acids from aspartic and glutamic acid derivatives

An efficient synthesis of enantiomerically pure β- and γ-amino acids starting from commercially available aspartic and glutamic acid derivatives is described. The acid function, α to the amino group, is first transformed to a good leaving group and the pr