100117-48-4

Upstream product

• 62926-84-5 1-(4-allylphenyl)ethanone 
• 1821-12-1 4-Phenylbutyric acid 
• 10031-93-3 ethyl 4-phenylbutyrate 
• 71665-59-3 4-(4-acetylphenyl)butyric acid ethyl ester 

Downstream Products

• 34162-06-6 4-(3-carboxypropyl)benzoic acid 
• 106949-28-4 7-acetyl-3,4-dihydro-2H-naphthalen-1-one 
• 89781-52-2 8-oxo-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid 
• 100117-94-0 4-<4-(carboxymethyl)phenyl>butyric acid 

Relevant academic research and scientific papers

Carbonylative Transformation of Allylarenes with CO Surrogates: Tunable Synthesis of 4-Arylbutanoic Acids, 2-Arylbutanoic Acids, and 4-Arylbutanals

In this Communication, procedures for the selective synthesis of 4-arylbutanoic acids, 2-arylbutanoic acids, and 4-arylbutanals from the same allylbenzenes have been developed. With formic acid or TFBen as the CO surrogate, reactions proceed selectively and effectively under carbon monoxide gas-free conditions.

Synthesis of 1-tetralone derivatives using a Stille cross coupling/friedel crafts acylation sequence

An efficient method of synthesis of 1-tetralones has been achieved featuring a Stille cross-coupling reaction as the key step.

Enediyne derivatives useful for the synthesis of conjugates of methyltrithio antitumor agents

This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.

Selective κ-opioid agonists: Synthesis and structure-activity relationships of piperidines incorporating an oxo-containing acyl group

This study describes the synthesis and the structure-activity relationships (SARs) of the (S)-(-)-enantiomers of a novel class of 2- (aminomethyl)piperidine derivatives, using κ-opioid binding affinity and antinociceptive potency as the indices of biological activity. Compounds incorporating the 1-tetralon-6-ylacetyl residue (30 and 34-45) demonstrated an in vivo antinociceptive activity greater than predicted on the basis of their κ-binding affinities. In particular, (2S)-2-[(dimethylamino)methyl]- 1-[(5,6,7,8-tetrahydro-5-oxo-2-naphthyl)acetyl]piperidine (34) was found to have a potency similar to spiradoline in animal models of antinociception after subcutaneous administration, with ED50s of 0.47 and 0.73 μmol/kg in the mouse and in the rat abdominal constriction tests, respectively. Further in vivo studies in mice and/or rats revealed that compound 34, compared to other selective κ-agonists, has a reduced propensity to cause a number of κ-related side effects, including locomotor impairment/sedation and diuresis, at antinociceptive doses. For example, it has an ED50 of 26.5 μmol/kg sc in the rat rotarod model, exhibiting a ratio of locomotor impairment/sedation vs analgesia of 36. Possible reasons for this differential activity and its clinical consequence are discussed.