5324-80-1

Upstream product

• 96-48-0 4-butanolide 
• 73632-20-9 sodium 1-naphthalenethiolate 
• 4897-84-1 Methyl 4-bromobutyrate 
• 91-60-1 2-Naphthalenethiol 
• 2623-87-2 bromobutyric acid 
• 39689-37-7 sodium salt of β-mercaptonaphthalene 
• 10442-65-6 ethyl 4-(2-naphthalenylthio)butanoate 
• 10442-62-3 3-(2-naphthythio)-1-propanol 
• 143-33-9 sodium cyanide 
• 727429-16-5 4-[2]naphthylsulfanyl-butyronitrile 

Relevant academic research and scientific papers

Aryl sulfones as novel Bradykinin B1 receptor antagonists for treatment of chronic pain

We report the development of aryl sulfones as Bradykinin B1 receptor antagonists. Variation of the linker region identified diol 23 as a potent B1 antagonist, while modifications of the aryl moiety led to compound 26, both of which were efficacious in rabbit biochemical challenge and pain models.

SUBSTITUTED SULFONES AND METHODS OF USE

Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Heterocyclic amines

Heterocyclic amines of the formula wherein Ar is a bicyclic or tricyclic aromatic group which is unsubstituted or which bears one or more substituents selected from halo, nitro and cyano groups and alkyl and alkoxy groups each of up to 4 carbon atoms; wherein X is a direct link or is --O--, --S--, --SO-- or --SO2 -- or has the formula --C(R3)=CH-- wherein R3 is hydrogen or alkyl of up to 4 carbon atoms; wherein A is straight or branched alkylene or alkenylene of 3 to 8 carbon atoms which may be interrupted by --O--, --S-- or --NH--; and wherein NR1 R2 is a cyclic amino group; or a pharmaceutically acceptable acid addition salt thereof, are of value for therapeutic use, particularly in the treatment of myocardial ischaemia and hypertension and in the treatment of fungal infections.

Ring Contraction of Some 1-Benzothiepin Derivatives to 1-Benzothiophens

Transformations of some 1-benzothiepin derivatives (1) into a 1-benzothiophen derivative (2a) through ring contraction are reported.Similar ring contraction of trans-1,2-dibromo-1,2,3,4-tetrahydronaphthothiepin (8) affords the thiophen derivative (9a).Treatment of the bromo-compounds (2a) and (9a) with base in the presence of catalysts provides in excelent yields the dienes (2d) and (9b) respectively.