75849-10-4

Upstream product

• 34708-60-6 3-(3-hydroxy-phenyl)propionic acid ethyl ester 
• 100-39-0 benzyl bromide 
• 14755-02-3 3-hydroxycinnamic acid 
• 208836-69-5 3-(3'-benzyloxyphenyl)-(E)-propenoic acid ethyl ester 
• 3943-96-2 3-(3-hydroxyphenyl)acrylic acid ethyl ester 
• 96251-92-2 (E)-3-(3-hydroxyphenyl)acrylic acid ethyl ester 
• 14755-02-3 3-hydroxy-trans-cinnamic acid 
• 621-54-5 3-(3-hydroxyphenyl)-propanoic acid 

Downstream Products

• 57668-35-6 3-[3-(Benzyloxy)phenyl]-1-propanol 
• 160721-33-5 ethyl 3-<3-(benzyloxy)phenyl>-2,2-dimethylpropanoate 
• 28495-92-3 5-(3-benzyloxy-benzyl)-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one 
• 121484-77-3 5-(2-(3-(3-benzyloxyphenyl)propamido)phenyl)-10,15,20-triphenylporphyrin 
• 121484-78-4 5-(2-(3-(3-hydroxyphenyl)propamido)phenyl)-10,15,20-triphenylporphyrin 
• 121484-76-2 3-(3-benzyloxy-phenyl)-propionyl chloride 
• 73087-65-7 1-(4-methoxyphenyl)-4-(3-methoxyphenyl)butan-1-ol 
• 75849-12-6 1-(2-benzyloxyphenyl)-4-(3-benzyloxyphenyl)butan-1-ol 
• 75849-22-8 1-(4-benzyloxyphenyl)-4-(3-benzyloxyphenyl)butan-1-ol 
• 73087-66-8 8-methoxy-1-(4-methoxyphenyl)-1,2,3,4-tetrahydronaphthalene 
• 75849-13-7 1-(2-methoxyphenyl)-4-(3-methoxyphenyl)butan-1-ol 
• 75849-11-5 1-(benzyloxy)-3-(3-bromopropyl)benzene 
• 73087-57-7 8-(2-Hydroxy-phenyl)-5,6,7,8-tetrahydro-naphthalen-1-ol 
• 73087-58-8 5-(2-Hydroxy-phenyl)-5,6,7,8-tetrahydro-naphthalen-2-ol 

Relevant academic research and scientific papers

MEDICINAL COMPOSITIONS IMPROVED IN SOLUBLITY IN WATER

Solid dispersions are provided comprising an HER2 inhibitor which is hardly or not soluble in water and a hydrophilic polymer. These solid dispersions have been improved in the solubility of the HER2 inhibitor, oral absorption and bioavailability in blood

MEDICINAL COMPOSITIONS HAVING IMPROVED ABSORBABILITY

An HER2 inhibitor having an average particle size of about 3 μm or less or a composition containing the same which has improved HER2 inhibitor-absorbability.

Inhibition of uridine phosphorylase: Synthesis and structure-activity relationships of aryl-substituted 5-benzyluracils and 1-[(2- hydroxyethoxy)methyl]-5-benzyluracils

A series of 1-[(2-hydroxyethoxy)methyl]-5-benzyluracils were synthesized and tested for inhibition of murine liver uridine phosphorylase (UrdPase). Inhibitors of UrdPase are reported to enhance the chemotherapeutic utility of 5-fluoro-2'-deoxyuridine and 5-fluorouracil and to ameliorate zidovudine- induced anemia in animal models. We prepared a series of 5-aryl-substituted analogues of 5-benzylacyclouridine (BAU), a good inhibitor of UrdPase (IC50 of 0.46 μM), to develop a compound with enhanced potency and improved pharmacokinetics. The first phase of structure-activity relationship studies on a series of 32 aryl-substituted 5-benzyluracils found several 5-(3- alkoxybenzyl) analogues of 5-benzyluracil with enhanced potency. The acyclovir side chain, the (2-hydroxyethoxy)methyl group, was substituted on the more potent aryl-substituted 5-benzyluracils. The two most potent compounds, 10y (3-propoxy) and 10dd (3-sec-butoxy), were inhibitors of UrdPase with IC50s of 0.047 and 0.027 μM, respectively. Six compounds were tested in vivo for effects on steady-state concentrations of circulating uridine in rats. Plasma uridine levels were elevated 3-9-fold by compound levels that ranged from 8 to 50 μM.

Regioselective synthesis of 1,8-dihydroxytetralins through a tandem reduction/intramolecular hydroxyalkylation of 4-(3-hydroxyphenyl)alkanoates

A series of 4-(3-hydroxyphenyl)butanoates 3 has been prepared and transformed into 1,8-dihydroxytetralins of general formula 2 by treatment with 2 equivalents of DIBALH followed by quenching with aqueous NH4Cl. A possible mechanism for this novel totally regioselective intramolecular hydroxyalkylation is suggested and the factors affecting the stability of 1,8-dihydroxytetralins 2 are also discussed.

Tandem Reduction / Intramolecular Hydroxyalkylation of (3-Hydroxyphenyl)alkanoates: a New Regioselective Approach to 1,8-Dihydroxytetralins

4-(3-hydroxyphenyl)-butanoates 4, on treatment with DIBALH, followed by hydrolytic work-up, undergo a novel completely regioselective intramolecular hydroxyalkylation reaction to give 1,8-dihydroxytetralins.The yield of the reaction depends heavily on the structure of starting material, best results being achieved with 3,3-disubstituted butanoates.

SYNTHESIS AND CHEMISTRY OF AN IRON(III) TETRAPHENYLPORPHYRIN WITH A COVALENTLY-ATTACHED PHENOLATE TAIL

We report the synthesis of a phenolate-tailed iron(III) tetraphenylporphyrin, 1.The phenolate ligand is covalently-attached to the porphyrin ring and is coordinated to the iron(III) center.This phenolate ligand increases the rate of oxygen atom transfer to the metal center.

PHENYL ALKYLAMINOPYRIMIDONES

The compounds are phenyl alkylaminopyrimidones which are histamine H. sub.2-antagonists. A specific compound of the present invention is 2-[2-[3-(dimethylaminomethyl)benzylthio]ethylamino]-5-(6-methyl-3-pyridylme thyl)-4-pyrimidone.

GUANIDINOTHIAZOLYL DERIVATIVES

The compounds are guanidinothiazolyl derivatives which are histamine H. sub.2-antagonists. A specific compound of the present invention is 2-2-(2-guanidino-4-thiazolylmethylthio)ethylamino!-5-(6-methyl-3-pyridylmethy l)-4-pyrimidone.

ISOUREAS AND ISOTHIOUREAS

The compounds are isoureas and isothioureas which have an O-or S-alkylpyrimidone substituent and which are histamine H 2-antagonists and antiinflammatory agents. A specific compound of this invention is 2-[5-(O-isoureido)pentylamino]-5-(6-methyl-3-pyridylmethyl)-4-pyrimidone.