69914-21-2

Usage

Uses

Used in Pharmaceutical Industry:
1-(2-hydroxy-2-phenylethyl)pyridin-2(1H)-one is used as a therapeutic agent for the treatment and prevention of osteoporosis in postmenopausal women. As a SERM, it helps to maintain bone density and reduce the risk of bone fractures by mimicking the effects of estrogen on bone tissue.
Additionally, raloxifene is used as a preventive measure for invasive breast cancer in postmenopausal women with osteoporosis. Its anti-cancer properties have shown potential in reducing the risk of developing breast cancer, making it a valuable addition to the arsenal of cancer prevention strategies.
Furthermore, raloxifene has been investigated for its potential applications in other areas, such as cardiovascular health and the treatment of certain types of cancer. However, more research is needed to fully understand its potential benefits and limitations in these areas.

Upstream product

• 952-75-0 1-(2-oxo-2-phenylethyl)-1,2-dihydropyridin-2-one 
• 67-56-1 methanol 
• 127074-84-4 1-(2-Hydroxy-2-phenylethyl)-4-piperidinol 
• 127074-72-0 1-Phenyl-2-(1,2,3,6-tetrahydropyridin-1-yl)-ethanol 
• 127074-85-5 2-(4-Piperidino-piperidino)-1-phenyl-ethanol 
• 96-09-3 styrene oxide 
• 63888-22-2 benzyl benzoylacetate 
• 614-27-7 methyl 3-oxo-3-phenylpropionate 
• 98-86-2 acetophenone 
• 504-29-0 2-aminopyridine 
• 532-27-4 1-chloroacetophenone 
• 127074-91-3 2-(4-Piperidino-piperidino)-1-phenyl-ethanon 
• 4897-50-1 4-piperidinopiperidin 
• 142-08-5 2-hydroxypyridin 

Relevant academic research and scientific papers

Route exploration and synthesis of the reported pyridone-based PDI inhibitor STK076545

The enzyme protein disulfide isomerase (PDI) is essential for the correct folding of proteins and the activation of certain cell surface receptors, and is a promising target for the treatment of cancer and thrombotic conditions. A previous high-throughput screen identified the commercial compound STK076545 as a promising PDI inhibitor. To confirm its activity and support further biological studies, a resynthesis was pursued of the reported β-keto-amide with an N-alkylated pyridone at the α-position. Numerous conventional approaches were complicated by undesired fragmentations or rearrangements. However, a successful 5-step synthetic route was achieved using an aldol reaction with an α-pyridone allyl ester as a key step. An X-ray crystal structure of the final compound confirmed that the reported structure of STK076545 was achieved, however its lack of PDI activity and inconsistent spectral data suggest that the commercial structure was misassigned.

Synthetic access to new pyridone derivatives through the alkylation reactions of hydroxypyridines with epoxides

General methods for the preparation of a variety of pyridone and oxypyridine derivatives are described. 2-,3-,4-Hydroxy pyridine and 2-pyridinemethanol were alkylated with ethylene-, propylene-, and stryrene-oxide and epichlorohydrin in the presence of di

Sodium mercury edetate dehydrogenation of N-aliphatic substituted 1,2,3,6-tetrahydropyridine derivatives

Hg(II)-edta dehydrogenation of N-aliphatic substituted Δ3-piperideine 1 leads to polymers. From 4 carrying a hydroxy neighbour group in the aliphatic side chain, it is possible to yield definite oxidation products - in dependence of nucleophiles present - mainly 4-substituted piperidone-2 derivatives 5 and 9-12. The oxidation of corresponding 4-hydroxy- (19) or 4-amino- (20, 21) piperidines gives the same spectrum of products. A mechanism for all the reactions is proposed.