34722-44-6

Upstream product

• 2365-48-2 Methyl thioglycolate 
• 105-13-5 4-Methoxybenzyl alcohol 
• 67-56-1 methanol 
• 34722-37-7 (4-methoxy-benzylsulfanyl)-acetic acid 
• 6258-60-2 p-methoxybenzylmercaptan 
• 89238-99-3 O-(4-methoxybenzyl)-trichloroacetimidate 
• 105-36-2 ethyl bromoacetate 

Downstream Products

• 108197-16-6 Diazo-(4-methoxy-phenylmethanesulfonyl)-acetic acid methyl ester 
• 515824-65-4 2-methylsulphenyl-4-hydroxy-5-(4-methoxybenzylsulphenyl)-pyrimidine 
• 122505-01-5 (4-Methoxy-phenylmethanesulfonyl)-acetic acid methyl ester 

Relevant academic research and scientific papers

Substituted α-mercaptoketones, new types of specific neprilysin inhibitors

New neprilysin inhibitors containing an α-mercaptoketone HSC(R1R2)CO group, as zinc ligand were designed. Two parameters were explored for potency optimization: the size of the inhibitor which could interact with the S1, S

MIXED INHIBITORS OF AMINOPEPTIDASE N AND NEPRILYSIN

Mixed inhibitors of aminopeptidase N and neprilysin are disclosed. Pharmaceutical compositions containing at least one of these compounds, used alone or in combination with morphine and derivatives thereof, endocannabinoids and inhibitors of endocannabinoid metabolism, GABA derivatives such as gabapentin or pregabalin, duloxetine or methadone, can be used as an analgesic, anxiolytic, antidepressant or anti-inflammatory.

Alkylation of thiols with trichloroacetimidates under neutral conditions

Trichloroacetimidates are displaced with thiols to form the corresponding sulfides without the need for an added acid or base by simply heating the reactants in refluxing THF. This operationally simple procedure provides the corresponding sulfides in excellent yields with only the formation of the neutral trichloroacetamide as the side product. The imidate may also be formed in situ, allowing for a direct method for the formation of sulfides from alcohols. This reaction provides a general method for the synthesis of a variety of sulfides from inexpensive and readily available alcohol starting materials.

3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase

The present invention relates to certain novel 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.

1-Carboxymethyl-2-oxo-azepan derivatives useful as selective inhibitors of MMP-12

The present invention relates to certain novel 1-carboxymethyl-2-oxo-azepan derivatives of the formula useful as inhibitors of matrix metalloproteinases (MMPs). The compounds of formula (1) are especially useful as selective inhibitors of MMP-12. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.

Intramolecular rhodium carbenoid insertions into aromatic C-H bonds. Preparation of 1,3-dihydrothiophene 2,2-dioxides fused onto aromatic rings

The preparation of 1-carboalkoxy-1,3-dihydrobenzenothiophene 2,2-dioxides via rhodium acetate or rhodium trifluoro-acetate catalyzed decomposition of α-diazo-β-arylmethanesulfonyl esters is described.The reaction has been extended to yield 1,3-dihydrothiophene 2,2-dioxides fused to the 2,3 position of thiophene and indole, but not of furans.In the latter case products derived from the opening of the furan ring were obtained.Key words: synthesis, 1-carboalkoxy-1,3-dihydrobenzothiophene 2,2-dioxides, intramolecular carbenoid insertions, rhodium acetate catalysis.